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70 kDa zeta-associated protein
-
-
-
-
A-Raf proto-oncogene serine/threonine-protein kinase
Abelson murine leukemia viral homolog (1) protein
Abelson tyrosine kinase
-
-
Abl nonreceptor tyrosine kinase
-
-
Abl protein tyrosine kinase
ABL2/ARG tyrosine kinase
-
-
activated Cdc42-associated tyrosine kinase 1
-
activin receptor type IIA
-
activin receptor type IIB
Agammaglobulinaemia tyrosine kinase
-
-
-
-
Amylovoran biosynthesis membrane-associated protein amsA
-
-
-
-
anti-mullerian hormone type II receptor
B lymphocyte kinase
-
-
-
-
B-cell/myeloid kinase
-
-
-
-
B-Raf proto-oncogene serine/threonine-protein kinase
-
BMP-2/BMP-4 receptor
-
-
-
-
Bone marrow kinase BMX
-
-
-
-
bone morphogenetic protein receptor type IA
bone morphogenetic protein receptor type IB
bone morphogenetic protein receptor type II
-
Bruton's tyrosine kinase PH domain
-
Brutons tyrosine kinase
-
-
c-Fes protein-tyrosine kinase
-
-
c-Fes tyrosine kinase
-
-
c-Src nonreceptor tyrosine kinase
-
-
c-Src protein tyrosine kinase
-
-
Calcium-dependent tyrosine kinase
-
-
-
-
calcium-dependent tyrosine kinase PYK2
-
-
CARD-containing interleukin-1 beta converting enzyme associated kinase
-
Cell adhesion kinase beta
-
-
-
-
cell-surface receptor daf-1
-
cell-surface receptor daf-4
-
cellular form of the transforming agent of Rous sarcoma virus
-
-
Csk homologous kinase
-
-
Csk protein-tyrosine kinase
-
-
CSK-homologous kinase
-
-
cytoplasmic protein tyrosine kinase
-
-
cytoplasmic tyrosine-protein kinase BMX
-
EC 2.7.1.112
-
-
formerly, part transferred
-
ectoprotein kinase
-
-
-
-
Epithelial and endothelial tyrosine kinase
-
-
-
-
EPS I polysaccharide export protein epsB
-
-
-
-
Fer protein-tyrosine kinase
-
-
focal adhesion kinase 1
-
-
-
-
focal adhesion protein tyrosine
Fps/Fes protein-tyrosine kinase
-
-
Fps/Fes tyrosine kinase
-
-
gene lck protein kinase
-
-
-
-
gene lck tyrosine kinase
-
-
-
-
hck-tr
truncated form of the src-related tyrosine kinase hck
Hematopoietic consensus tyrosine-lacking kinase
Hemopoietic cell kinase
-
-
-
-
IL-1R-associated kinase
-
IL-2-inducible T-cell kinase
-
-
-
-
integrin-linked protein kinase
-
integrin-linked protein kinase 1
-
integrin-linked protein kinase 76
-
interleukin-1 receptor-associated kinase 1
interleukin-1 receptor-associated kinase-81
-
JAK protein tyrosine kinase
-
-
-
-
JAK2 protein tyrosine kinase
-
Janus family kinase JAK3
-
just another kinase 2
-
-
kinase, protein (phosphorylating tyrosine)
-
-
-
-
kinase, protein p56lck (phosphorylating)
-
-
-
-
Lck Tyrosine kinase
-
-
-
-
lymphocyte-specific protein tyrosine kinase
Lyn protein tyrosine kinase
-
-
megakaryocyte-associated tyrosine-protein kinase
mullerian inhibiting substance type II receptor
-
neuronal proto-oncogene tyrosine-protein kinase SRC
-
non-receptor membrane-associated PTK
-
-
non-receptor protein tyrosine kinase
non-receptor protein-tyrosine kinase
-
-
non-receptor tyrosine kinase
non-receptor tyrosine kinase ABL
-
non-receptor tyrosine kinase brk
-
non-receptor tyrosine-protein kinase TYK2
nonreceptor protein tyrosine kinase
-
-
-
-
nonreceptor protein tyrosine kinase Pyk2
-
nonreceptor tyrosine kinase
nonreceptor tyrosine kinase c-Abl
-
nonreceptor tyrosine kinase Fes
-
nonreceptor tyrosine kinase Src
-
nonreceptor tyrosine kinase Srm
-
nonreceptor tyrosine kinase SYK
nonreceptor tyrosine kinase Tec
-
Nuclear tyrosine protein kinase RAK
-
-
-
-
p135tyk2 tyrosine kinase
-
p56lck protein kinase
-
-
-
-
p56lck protein tyrosine kinase
-
-
-
-
p56lck tyrosine kinase
-
-
-
-
phosphotyrosyl-protein kinase
-
-
-
-
proline-rich tyrosin ekinase 2
-
-
proline-rich tyrosine kinase 2
proline-rich tyrosine kinase-2
-
-
Protein kinase (tyrosine-phosphorylating)
-
-
-
-
Protein kinase BATK
-
-
-
-
Protein kinase HYL
-
-
-
-
Protein kinase Lck
-
-
-
-
Protein kinase NTK
-
-
-
-
Protein kinase p56-LCK
-
-
-
-
Protein kinase p56lck
-
-
-
-
Protein p56c-lck kinase
-
-
-
-
Protein p56lck tyrosine kinase
-
-
-
-
protein tyrosine kinase 2
-
-
protein tyrosine kinase 2beta
-
-
-
-
protein tyrosine kinase 6
-
protein tyrosine kinase 70
-
protein tyrosine kinase focal adhesion kinase
-
-
Protein tyrosine kinase lck
-
-
-
-
Protein tyrosine kinase p56lck
-
-
-
-
Protein tyrosine kinase pp56lck
-
-
-
-
protein tyrosine kinase PTK70
-
protein-tyrosine kinase Brk
-
Protein-tyrosine kinase C-TKL
-
-
-
-
Protein-tyrosine kinase CYL
-
-
-
-
Protein-tyrosine kinase Syk
-
-
proto-oncogene serine/threonine-protein kinase mos
proto-oncogene tyrosine-protein kinase ABL1
proto-oncogene tyrosine-protein kinase FER
-
proto-oncogene tyrosine-protein kinase FES/FPS
proto-oncogene tyrosine-protein kinase FGR
-
proto-oncogene tyrosine-protein kinase FYN
proto-oncogene tyrosine-protein kinase LCK
proto-oncogene tyrosine-protein kinase SRC
proto-oncogene tyrosine-protein kinase YES
proto-oncogene tyrosine-protein kinase YRK
-
RAF homolog serine/threonine-protein kinase dRAF-1
-
RAF proto-oncogene serine/threonine-protein kinase
receptor interacting protein 3
receptor protein kinase CLAVATA1 precursor
-
receptor-associated kinase JAK2
-
receptor-interacting serine/threonine protein kinase 2
receptor-interacting serine/threonine protein kinase 3
-
receptor-like protein kinase 5 precursor
-
Related adhesion focal tyrosine kinase
-
-
-
-
Resting lymphocyte kinase
S-domain receptor-like protein kinase
-
-
-
-
serine/threonine kinase receptor
-
serine/threonine protein kinase mos
-
serine/threonine-protein kinase receptor R2
serine/threonine-protein kinase receptor R3
serine/threonine-protein kinase receptor TKV
-
serine/threonine-protein kinase sma-6
-
serine/threonine-protein kinase transforming protein mos
serine/threonine-protein kinase transforming protein raf
-
Src family tyrosine kinase Lyn
-
Src protein tyrosine kinase
-
-
src protein tyrosine kinase p56Lck
-
-
Src protein-tyrosine kinase
Src-family protein kinase
-
Src-family protein tyrosine kinase
-
-
SRC-related intestinal kinase
Syk-related tyrosine kinase
-
-
-
-
T cell-specific protein-tyrosine kinase
-
-
-
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T-cell-specific kinase
-
-
-
-
Tec family tyrosine kinase
-
-
testis-specific protein kinase 1
testis-specific protein kinase 2
TGF-beta receptor type II
TGF-beta type II receptor
-
transforming agent of Fujinami sarcoma virus
-
-
transforming growth factor beta type II receptor
-
transforming growth factor-beta type I receptor 7
-
Tyrosine kinase ARG
-
-
-
-
tyrosine kinase c-Src
-
-
Tyrosine kinase lck
-
-
-
-
Tyrosine kinase p56lck
-
-
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-
tyrosine kinase p60c-src
-
-
tyrosine kinase sf-Stk
-
-
Tyrosine phosphokinase
-
-
-
-
Tyrosine protein kinase
-
-
-
-
Tyrosine protein kinase p56lck
-
-
-
-
tyrosine-protein kinase 6
tyrosine-protein kinase Abl
-
tyrosine-protein kinase abl-1
-
tyrosine-protein kinase ABL2
-
tyrosine-protein kinase BLK
Tyrosine-protein kinase brk
-
-
-
-
tyrosine-protein kinase BTK
tyrosine-protein kinase CSK
Tyrosine-protein kinase CTK
-
-
-
-
tyrosine-protein kinase Fps85D
-
tyrosine-protein kinase FRK
-
tyrosine-protein kinase HCK
tyrosine-protein kinase hopscotch
-
tyrosine-protein kinase HTK16
-
tyrosine-protein kinase ITK/TSK
tyrosine-protein kinase JAK1
tyrosine-protein kinase JAK2
tyrosine-protein kinase JAK3
Tyrosine-protein kinase Lyk
-
-
-
-
tyrosine-protein kinase LYN
tyrosine-protein kinase PR2
-
tyrosine-protein kinase shark
-
tyrosine-protein kinase SPK-1
-
tyrosine-protein kinase SRC-1
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tyrosine-protein kinase SRC-2
-
tyrosine-protein kinase Src42A
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tyrosine-protein kinase Src64B
-
tyrosine-protein kinase SRK1
-
tyrosine-protein kinase SRK4
-
tyrosine-protein kinase SRM
-
tyrosine-protein kinase STK
-
tyrosine-protein kinase SYK
tyrosine-protein kinase Tec
tyrosine-protein kinase transforming protein ABL
tyrosine-protein kinase transforming protein FES
tyrosine-protein kinase transforming protein FGR
tyrosine-protein kinase transforming protein fms
tyrosine-protein kinase transforming protein FPS
tyrosine-protein kinase transforming protein ros
tyrosine-protein kinase transforming protein SEA
tyrosine-protein kinase transforming protein SRC
tyrosine-protein kinase transforming protein YES
tyrosine-protein kinase TXK
Tyrosine-protein kinase TYRO 10
-
-
-
-
tyrosine-protein kinase ZAP-70
Tyrosine-specific protein kinase
-
-
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Tyrosylprotein kinase
-
-
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v-fps Protein-tyrosine kinase
-
-
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YES related kinase
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-
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A-Raf proto-oncogene serine/threonine-protein kinase
-
A-Raf proto-oncogene serine/threonine-protein kinase
-
A-Raf proto-oncogene serine/threonine-protein kinase
-
A-Raf proto-oncogene serine/threonine-protein kinase
-
Abelson murine leukemia viral homolog (1) protein
-
-
Abelson murine leukemia viral homolog (1) protein
-
-
Abl
-
-
Abl kinase
-
-
Abl protein tyrosine kinase
-
-
Abl protein tyrosine kinase
-
Abl tyrosine kinase
Abelson leukaemia virus
-
-
Abl tyrosine kinase
-
present in 95% of patients with chronic myelogenous leukemia, CML
ABL1
-
-
ABL2
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ACK1
-
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activin receptor type I
-
activin receptor type I
-
activin receptor type I
-
activin receptor type II
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activin receptor type II
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activin receptor type II
-
activin receptor type II
-
activin receptor type II
-
activin receptor type IIB
-
activin receptor type IIB
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activin receptor type IIB
-
ACTR-IIB
-
-
-
-
AKT
-
-
anti-mullerian hormone type II receptor
-
anti-mullerian hormone type II receptor
-
B cell progenitor kinase
-
-
-
-
B cell progenitor kinase
-
BCR-ABL tyrosine kinase
-
-
-
-
BCR-ABL tyrosine kinase
-
-
BCR/ABL kinase
-
-
Blk
-
-
BMP type II receptor
-
-
-
-
Bmx
-
-
bone morphogenetic protein receptor type IA
-
bone morphogenetic protein receptor type IA
-
bone morphogenetic protein receptor type IB
-
bone morphogenetic protein receptor type IB
-
bone morphogenetic protein receptor type IB
-
Breast tumor kinase
-
-
-
-
Brk
-
-
Bruton tyrosine kinase
-
Bruton's tyrosine kinase
-
-
-
-
Bruton's tyrosine kinase
-
-
Bruton's tyrosine kinase
-
Bruton's tyrosine kinase
-
-
Bruton's tyrosine kinase
-
Brutons tyrosine kinase
-
-
Brutons tyrosine kinase
-
Brutons tyrosine kinase
-
-
Brutons tyrosine kinase
-
-
-
Btk
-
-
c-ABL
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-
-
-
c-Abl tyrosine kinase
-
-
c-Abl tyrosine kinase
-
isoforms 1a and 1b
C-SRC
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-
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C-SRC kinase
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-
-
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c-Src tyrosine kinase
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-
c-Src tyrosine kinase
-
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C-terminal Src kinase
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-
C-terminal Src kinase
-
-
C-YES
-
-
-
-
Csk
-
-
ETK
-
-
FAK
-
Fgr
-
-
focal adhesion kinase
-
focal adhesion protein tyrosine
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-
focal adhesion protein tyrosine
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-
FRK
-
-
Fyn
-
-
HCK
-
-
Hematopoietic consensus tyrosine-lacking kinase
-
-
-
-
Hematopoietic consensus tyrosine-lacking kinase
-
interleukin-1 receptor-associated kinase 1
-
interleukin-1 receptor-associated kinase 1
-
Itk
-
-
-
-
JAK
-
-
Jak1
-
-
JAK2
-
-
JAK2
-
-
661392, 672954, 674865, 702439, 703984, 703985, 704787, 705448, 705664, 705895, 705943, 705953, 706405, 706765, 706766, 723583, 738741
Jak3
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-
Janus kinase
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-
Janus kinase
-
-
662571, 701645, 703984, 703985, 704787, 705664, 705895, 705953, 706405, 706765, 706766
Janus kinase 1
-
-
Janus kinase 2
-
-
Lck
-
-
Leukocyte janus kinase
-
-
-
-
LIM domain kinase 2
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lymphocyte-specific protein tyrosine kinase
-
-
lymphocyte-specific protein tyrosine kinase
-
-
Lyn
-
-
Lyn tyrosine kinase
-
megakaryocyte-associated tyrosine-protein kinase
-
megakaryocyte-associated tyrosine-protein kinase
-
non-receptor protein tyrosine kinase
-
-
non-receptor protein tyrosine kinase
-
-
non-receptor PTK
-
-
non-receptor tyrosine kinase
-
-
non-receptor tyrosine kinase
-
-
non-receptor tyrosine kinase
-
-
non-receptor tyrosine-protein kinase TYK2
-
non-receptor tyrosine-protein kinase TYK2
-
nonreceptor tyrosine kinase
-
-
nonreceptor tyrosine kinase
-
-
nonreceptor tyrosine kinase
-
nonreceptor tyrosine kinase
-
-
nonreceptor tyrosine kinase SYK
-
nonreceptor tyrosine kinase SYK
-
p40mos
-
p56lck
-
-
PP125FAK
-
-
-
-
proline-rich tyrosine kinase 2
-
-
proline-rich tyrosine kinase 2
-
Protein tyrosine kinase
-
-
-
-
Protein tyrosine kinase
-
-
Protein tyrosine kinase
-
Protein tyrosine kinase
-
-
660970, 661180, 661392, 661396, 661457, 661461, 661487, 661540, 661548, 661749, 662556, 662838, 662858, 663021, 663196, 663291, 674767, 690302
Protein tyrosine kinase
-
Protein tyrosine kinase
-
-
Protein tyrosine kinase
-
-
-
Protein tyrosine kinase
-
-
Protein tyrosine kinase
-
-
Protein tyrosine kinase
-
-
protein-tyrosine kinase
-
-
protein-tyrosine kinase
-
-
protein-tyrosine kinase
-
-
proto-oncogene serine/threonine-protein kinase mos
-
proto-oncogene serine/threonine-protein kinase mos
-
proto-oncogene serine/threonine-protein kinase mos
-
proto-oncogene serine/threonine-protein kinase mos
-
proto-oncogene tyrosine-protein kinase ABL1
-
490048, 490049, 490050, 490051, 490052, 490053, 490054, 490055, 490056, 490057, 490058, 490059
proto-oncogene tyrosine-protein kinase ABL1
-
proto-oncogene tyrosine-protein kinase FES/FPS
-
proto-oncogene tyrosine-protein kinase FES/FPS
-
proto-oncogene tyrosine-protein kinase FYN
-
proto-oncogene tyrosine-protein kinase FYN
-
proto-oncogene tyrosine-protein kinase FYN
-
proto-oncogene tyrosine-protein kinase FYN
-
proto-oncogene tyrosine-protein kinase LCK
-
proto-oncogene tyrosine-protein kinase LCK
-
proto-oncogene tyrosine-protein kinase LCK
-
490114, 490115, 490116, 490117, 490118, 490119, 490120, 490121, 490122, 490123, 490124
proto-oncogene tyrosine-protein kinase SRC
-
proto-oncogene tyrosine-protein kinase SRC
-
proto-oncogene tyrosine-protein kinase SRC
-
proto-oncogene tyrosine-protein kinase YES
-
proto-oncogene tyrosine-protein kinase YES
-
proto-oncogene tyrosine-protein kinase YES
-
proto-oncogene tyrosine-protein kinase YES
-
proto-oncogene tyrosine-protein kinase YES
-
proto-oncogene tyrosine-protein kinase YES
-
PTK
-
-
-
-
PTK
-
-
660885, 660970, 661180, 661392, 661396, 661457, 661461, 661487, 661540, 661548, 661749, 662556, 662838, 662858, 663021, 663291, 673223, 673959, 690302, 706765, 706766
PTK70
-
-
-
-
Pyk2
-
-
RAF proto-oncogene serine/threonine-protein kinase
-
RAF proto-oncogene serine/threonine-protein kinase
-
RAF proto-oncogene serine/threonine-protein kinase
-
receptor interacting protein 3
-
receptor interacting protein 3
-
receptor-interacting serine/threonine protein kinase 2
-
receptor-interacting serine/threonine protein kinase 2
-
receptor-interacting serine/threonine protein kinase 2
-
Resting lymphocyte kinase
-
-
-
-
Resting lymphocyte kinase
-
serine/threonine-protein kinase receptor R2
-
serine/threonine-protein kinase receptor R2
-
serine/threonine-protein kinase receptor R3
-
serine/threonine-protein kinase receptor R3
-
serine/threonine-protein kinase receptor R3
-
serine/threonine-protein kinase transforming protein mos
-
serine/threonine-protein kinase transforming protein mos
-
serine/threonine-protein kinase transforming protein mos
-
serine/threonine-protein kinase transforming protein mos
-
-
serine/threonine-protein kinase transforming protein mos
-
-
serine/threonine-protein kinase transforming protein mos
-
SFK
-
-
Spleen tyrosine kinase
-
-
-
-
Spleen tyrosine kinase
-
-
Spleen tyrosine kinase
-
-
Src
-
-
Src
-
-
660885, 660970, 661540, 662556, 663021, 663291, 671253, 672104, 676266, 703579, 737321, 738408, 738876
Src family kinase
-
-
Src kinase
-
-
Src protein-tyrosine kinase
-
-
Src protein-tyrosine kinase
-
-
Src protein-tyrosine kinase
-
-
Src tyrosine kinase
-
-
SRC-related intestinal kinase
-
-
-
-
SRC-related intestinal kinase
-
Syk
-
-
661457, 661749, 662174, 662858, 663021, 672781, 675097, 675205, 690415, 691312, 693315
Tec
-
-
Tec kinase
-
-
TESK2
-
testis-specific protein kinase 1
-
testis-specific protein kinase 1
-
testis-specific protein kinase 2
-
testis-specific protein kinase 2
-
TGF-beta receptor type I
-
TGF-beta receptor type I
-
TGF-beta receptor type I
-
TGF-beta receptor type II
-
TGF-beta receptor type II
-
TGF-beta receptor type II
-
Tyk2
-
-
tyrosine kinase Abl
-
-
tyrosine kinase Fyn
-
tyrosine kinase Src
-
-
tyrosine-protein kinase 6
-
tyrosine-protein kinase 6
-
tyrosine-protein kinase BLK
-
tyrosine-protein kinase BLK
-
tyrosine-protein kinase BTK
-
tyrosine-protein kinase BTK
-
tyrosine-protein kinase CSK
-
tyrosine-protein kinase CSK
-
tyrosine-protein kinase CSK
-
tyrosine-protein kinase CSK
-
tyrosine-protein kinase HCK
-
tyrosine-protein kinase HCK
-
tyrosine-protein kinase HCK
-
tyrosine-protein kinase HCK
-
tyrosine-protein kinase ITK/TSK
-
tyrosine-protein kinase ITK/TSK
-
tyrosine-protein kinase JAK1
-
tyrosine-protein kinase JAK1
-
tyrosine-protein kinase JAK1
-
tyrosine-protein kinase JAK1
-
tyrosine-protein kinase JAK2
-
tyrosine-protein kinase JAK2
-
tyrosine-protein kinase JAK2
-
tyrosine-protein kinase JAK3
-
tyrosine-protein kinase JAK3
-
tyrosine-protein kinase JAK3
-
tyrosine-protein kinase LYN
-
tyrosine-protein kinase LYN
-
tyrosine-protein kinase LYN
-
tyrosine-protein kinase SYK
-
tyrosine-protein kinase SYK
-
tyrosine-protein kinase SYK
-
tyrosine-protein kinase SYK
-
tyrosine-protein kinase Tec
-
tyrosine-protein kinase Tec
-
tyrosine-protein kinase transforming protein ABL
-
tyrosine-protein kinase transforming protein ABL
-
tyrosine-protein kinase transforming protein ABL
-
-
tyrosine-protein kinase transforming protein FES
-
tyrosine-protein kinase transforming protein FES
-
-
tyrosine-protein kinase transforming protein FES
-
-
tyrosine-protein kinase transforming protein FGR
-
tyrosine-protein kinase transforming protein FGR
-
-
tyrosine-protein kinase transforming protein fms
-
tyrosine-protein kinase transforming protein fms
-
-
tyrosine-protein kinase transforming protein FPS
-
tyrosine-protein kinase transforming protein FPS
-
-
tyrosine-protein kinase transforming protein FPS
-
tyrosine-protein kinase transforming protein ros
-
tyrosine-protein kinase transforming protein ros
-
-
tyrosine-protein kinase transforming protein SEA
-
tyrosine-protein kinase transforming protein SEA
-
-
tyrosine-protein kinase transforming protein SRC
-
tyrosine-protein kinase transforming protein SRC
-
tyrosine-protein kinase transforming protein SRC
-
tyrosine-protein kinase transforming protein SRC
-
-
tyrosine-protein kinase transforming protein SRC
-
-
tyrosine-protein kinase transforming protein SRC
-
-
tyrosine-protein kinase transforming protein SRC
-
tyrosine-protein kinase transforming protein SRC
-
tyrosine-protein kinase transforming protein SRC
-
tyrosine-protein kinase transforming protein SRC
-
tyrosine-protein kinase transforming protein SRC
-
-
tyrosine-protein kinase transforming protein SRC
-
-
tyrosine-protein kinase transforming protein YES
-
tyrosine-protein kinase transforming protein YES
-
-
tyrosine-protein kinase TXK
-
tyrosine-protein kinase TXK
-
tyrosine-protein kinase ZAP-70
-
tyrosine-protein kinase ZAP-70
-
v-Src
-
-
WEE1hu
-
-
-
-
Yes
-
-
yrk
-
additional information
-
the enzymes belong to the Src family of kinases
additional information
Yes kinase is a Src-family tyrosine kinase
additional information
-
the enzyme belongs to the Janus family of tyrosine kinases
additional information
-
Btk is a member of the Tec family of protein kinases
additional information
-
Chk belongs to the Src family of PTKs
additional information
-
Csk belongs to the Src kinase family
additional information
-
Fyn is a tyrosine protein kinase of the Src family
additional information
-
JAK2 is a member of the Janus kinase family of PTKs
additional information
-
Lck is a member of the Src non-receptor tyrosine kinase family
additional information
-
Lyn, Hck, and Pyk-2 belong to the Src family of PTKs
additional information
-
member of the Src kinase family
additional information
-
non-receptor PTKs are grouped into several families and subfamilies
additional information
-
Syk belongs to the Syk family of protein tyrosine kinases, Src and Lyn belong to the Src family of protein tyrosine kinases
additional information
-
Syk is a member of the tyrosine kinase family
additional information
-
Syk, Fyn, and Abl belong to the Src family of PTKs
additional information
-
Tec, Btk, Itk, and Bmx are members of the Tec tyrosine kinase family
additional information
-
the enzyme belongs to the Janus family of tyrosine kinases
additional information
-
the enzyme belongs to the protein tyrosine kinase family
additional information
-
the enzyme belongs to the Src subfamily of the protein tyrosine kinase family
additional information
-
the enzyme belongs to the Src tyrosine kinase family
additional information
-
the enzyme belongs to the Tec nonreceptor tyrosine kinase family
additional information
-
the enzyme is a member of the Src family of tyrosine kinases
additional information
-
the Src kinase family consists of protein kinases c-Src, Fyn, Lck, Yes, Lyn, Hck, Fgr, Blk, and Yrk
additional information
-
the Src kinase family contains 11 members, i.e. protein tyrosine kinases Blk, Brk, Fgr, Frk, Fyn, Hck, Lck, Lyn, Src, Srm, and Yes
additional information
-
ZAP-70 belongs to the Syk protein tyrosine kinase family
additional information
the enzyme belongs to the nonreceptor protein-tyrosine kinase, PTK, family
additional information
-
enzymes belonging to the Src kinase family
additional information
-
PTKs of the Src kinase family
additional information
-
the enzyme belongs to the Janus family of tyrosine kinases
additional information
-
the enzyme belongs to the Src subfamily of the protein tyrosine kinase family
additional information
the enzyme belongs to the Janus family of tyrosine kinases
additional information
-
PTKs of the Src kinase family
-
additional information
-
the enzyme belongs to the Src tyrosine kinase family
additional information
-
member of the Src kinase family
additional information
-
the enzyme belongs to the Src subfamily of the protein tyrosine kinase family
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AEEEIYGEFEAKKKK + ATP
? + ADP
-
-
-
?
ATP + a protein
ADP + a phosphoprotein
ATP + a [homeodomain-interacting protein kinase 2]-L-tyrosine
ADP + a [homeodomain-interacting protein kinase 2]-L-tyrosine phosphate
-
-
-
-
?
ATP + a [peptide]-L-tyrosine
ADP + a [peptide]-L-tyrosine phosphate
-
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
ATP + a [Tyr-2 peptide]-L-tyrosine
ADP + a [Tyr-2 peptide]-L-tyrosine phosphate
-
-
-
?
ATP + A-kinase anchor protein 8
?
-
-
-
-
?
ATP + Abl
ADP + phospho-L-tyrosinyl-Abl
ATP + Akt tyrosine kinase
ADP + phosphotyrosinyl-Akt
ATP + arsenate resistance protein ARS2
?
-
-
-
-
?
ATP + ataxin 2 related protein
?
-
-
-
-
?
ATP + Bad protein
ADP + phosphotyrosinyl Bad protein
ATP + Bcl-2-associated transcription factor 1
?
-
-
-
-
?
ATP + beta 1-integrin cytoplasmic domain peptide
ADP + ?
-
-
-
?
ATP + beta-catenin
ADP + phospho-tyrosinyl-beta-catenin
ATP + biotin-GGEAIYAAPFKK-amide
ADP + phosphorylated biotin-GGEAIYAAPFKK-amide
-
a peptide with the preferred c-Abl substrate sequence carrying an Nterminal biotin
-
-
?
ATP + calponin 3
?
-
-
-
-
?
ATP + Cas protein
ADP + phospho-tyrosinyl-Cas protein
ATP + casein
ADP + phosphocasein
serine/threonine kinase activity, and no tyrosine kinase activity
-
-
?
ATP + Cbp
? + ADP
-
murine Csk binding protein, Cbp, amino acids 74-474, substrate used in kinase activity assay
-
-
?
ATP + cdc2
ADP + phosphorylated cdc2
ATP + cdc2(6-20) peptide
?
-
i.e. KVEKIGEGTYGVVYK, substrate of Src family kinases
-
-
?
ATP + chromosome 20 open reading frame 77
?
-
-
-
-
?
ATP + cleavage and polyadenylation specific factor 5
?
-
-
-
-
?
ATP + cofilin
ADP + phosphorylated cofilin
ATP + cortactin
?
-
-
-
-
?
ATP + cortactin
ADP + phospho-tyrosinyl-cortactin
ATP + cyclin-associated cyclin-dependent kinase
ADP + phosphorylated cyclin-associated cyclin-dependent kinase
ATP + EAIYAAPFAKKKG
ADP + EAI-pY-AAPFAKKKG
-
-
-
-
?
ATP + EEEEY
ADP + EEEE(phospho)Y
-
-
-
-
?
ATP + EEEEYIQ[dP]-8-hydroxy-5-(N,N-dimethylsulfonamido)-2-methylquinoline-G
ADP + EEEEYIQ[dP]-8-hydroxy-5-(N,N-dimethylsulfonamido)-2-methylquinoline-G phosphate
-
Y7 Sox-based substrate, kinetic assay
-
-
?
ATP + EEEPQYEEIPI +
ADP + EEEPQpYEEIPI
-
-
-
-
?
ATP + enolase
ADP + ?
serine/threonine kinase activity, and no tyrosine kinase activity
-
-
?
ATP + epidermal growth factor receptor
ADP + phospho-L-tyrosinyl-epidermal growth factor receptor
ATP + EQEDEPEGDYFEWLE
ADP + EQEDEPEGDpYFEWLE
-
-
-
-
?
ATP + eukaryotic translation initiation factor 3, subunit 4
?
-
-
-
-
?
ATP + ewing sarcoma breakpoint region 1
?
-
-
-
-
?
ATP + ezrin
ADP + phospho-tyrosinyl-ezrin
ATP + F peptide
ADP + phospho-L-tyrosinyl-F peptide
-
i.e. biotin-Aca-AAAEEIFGEI-NH2
-
-
?
ATP + FAK
ADP + phospho-tyrosinyl-FAK
ATP + FUS interacting protein (serine/arginine rich) 1
?
-
-
-
-
?
ATP + FUS/TLS oncogene
?
-
-
-
-
?
ATP + FUSE binding protein
?
-
-
-
-
?
ATP + FUSE binding protein 2
?
-
-
-
-
?
ATP + GAPEVIYATPGAKKK
ADP + GAPEVI-phosphotyrosinyl-ATPGAKKK
-
consensus substrate
-
-
?
ATP + GGEAIYAAPFKK
ADP + GGEAIYAAPFKK phosphate
-
kinase assay using biotinylated model substrate peptide
-
-
?
ATP + glycogen synthase kinase 3beta
ADP + phosphotyrosinyl glycogen synthase kinase 3beta
ATP + heterogeneous nuclear ribonucleoprotein A3
?
-
-
-
-
?
ATP + heterogeneous nuclear ribonucleoprotein AB
?
-
-
-
-
?
ATP + heterogeneous nuclear ribonucleoprotein D-like
?
-
-
-
-
?
ATP + heterogeneous nuclear ribonucleoprotein K
?
-
-
-
-
?
ATP + histone
ADP + phosphorylated histone
serine/threonine-specific kinase activity
-
-
?
ATP + homeobox prox 1
?
-
-
-
-
?
ATP + IkappaBalpha-L-tyrosine
ADP + IkappaBalpha-L-tyrosine phosphate
ATP + KVEKIGEGTYGVVYK
? + ADP
substrate peptide used in kinase activity assay, derived from p34cdc2
-
-
?
ATP + KVEKIGEGTYGVVYK
ADP + ?
-
synthetic peptide substrate
-
-
?
ATP + lysozyme-L-tyrosine
ADP + lysozyme-L-tyrosine phosphate
-
substrate of Src, low activity with Csk or Chk
-
-
?
ATP + myelin basic protein
ADP + ?
-
-
-
?
ATP + myelin basic protein
ADP + phosphorylated myelin basic protein
ATP + myosin light chain
ADP + ?
serine/threonine kinase activity, and no tyrosine kinase activity
-
-
?
ATP + NaV1.2 channel
ADP + phospho-L-tyrosinyl-NaV1.2 channel
-
Y66 and Y1893, which are in consensus sequences appropriate for binding to the Fyn SH2 domain after phosphorylation, are both required for optimal binding and regulation by Fyn. Y730, which is located near the SH3-binding motif in LI-II, and Y1497 and Y1498 in the inactivation gate in LIII-IV, are also required for optimal regulation, but phosphorylation of these sites likely promotes fast inactivation
-
-
?
ATP + NEFA-interacting nuclear protein
?
-
-
-
-
?
ATP + P1 peptide
ADP + phospho-L-tyrosinyl-P1 peptide
-
i.e. biotin-Aca-AAAEEIpYGEI-NH2
-
-
?
ATP + p120 protein
ADP + phospho-tyrosinyl-p120 protein
ATP + p190 GTPase
ADP + phospho-tyrosinyl-p190 GTPase
ATP + p32-L-tyrosine
ADP + p32-L-tyrosine phosphate
ATP + p34cdc2
ADP + phosphorylated p34cdc2
ATP + PAK1
ADP + phospho-L-tyrosinyl-PAK1
ATP + paxillin
ADP + phospho-tyrosinyl-Shc paxillin
ATP + peptide
ADP + phospho-L-tyrosinyl-peptide
-
PTKs phosphorylate substrates in a sequence-specific manner, relatively short peptide sequences determine selectivity, substrate specificity analysis using 144 different peptides, overview
-
-
?
ATP + PIKE-A
ADP + phosphotyrosinyl-PIKE-A
ATP + plakoglobin
ADP + phospho-tyrosinyl-plakoglobin
ATP + poly(Glu,Tyr)
? + ADP
substrate used in the tyrosine kinase asssay
-
-
?
ATP + poly(Glu-Tyr)
? + ADP
-
substrate used in the activity assay
-
-
?
ATP + poly(Glu4-Tyr)
ADP + poly(Glu4-Tyr)-L-tyrosine phosphate
ATP + poly-(Tyr-Glu)
ADP + phospho-poly-(Tyr-Glu)
-
tyrosine kinase substrate, phosphoryated by Swe1p, Mps1p, Ime2p, and Hrr25p, but not by Ste7p, Rad53p, or Mck1p
-
-
?
ATP + proteasome activator subunit 3
?
-
-
-
-
?
ATP + protein
?
CSK phosphorylates other members of the src-family of tyrosine kinases at their regulatory carboxy-terminus. By regulating the activity of these kinases, CSK may play an important role in cell growth and development
-
-
?
ATP + protein
ADP + protein tyrosine phosphate
ATP + protein tyrosine
ADP + protein tyrosine phosphate
ATP + protein tyrosine kinase Yes
ADP + phospho-L-tyrosinyl Yes
-
Csk inactivates the enzyme substrate
-
-
?
ATP + RasGAP SH3-domain binding protein
?
-
-
-
-
?
ATP + recombinant GST/beta3 integrin cytoplasmic tail peptide
ADP + ?
-
-
-
?
ATP + Rho protein
ADP + phospho-tyrosinyl-Rho protein
ATP + RNA binding motif protein 10
?
-
-
-
-
?
ATP + RNA binding motif protein 4B
?
-
-
-
-
?
ATP + S1 peptide
ADP + phospho-L-tyrosinyl-S1 peptide
-
i.e. biotin-Aca-AAAEEIYGEI-NH2
-
-
?
ATP + Shc protein
ADP + phospho-tyrosinyl-Shc protein
ATP + signal transducer and activator of transcription
ADP + phospho-L-tyrosinyl-signal transducer and activator of transcription
ATP + similar to zinc finger CCCH-type domain-containing protein 6
?
-
-
-
-
?
ATP + splicing factor proline/glutamine-rich
?
-
-
-
-
?
ATP + splicing factor, arginine/serine-rich9
?
-
-
-
-
?
ATP + Src
ADP + phospho-L-tyrosinyl Src family kinase
-
wild-type Src and catalytically inactive mutant Src K295M, terminal Src kinase Csk specifically phosphorylates Src family kinases on a C-terminal Tyr residue, which down-regulates their activities, identification of the docking determinants in Src recognized by the Csk substrate-docking site, Glu510 of Src interacts with Arg283 of Csk in Csk-Src recognition, activity with Src fragments, overview
-
-
?
ATP + Src family kinase
?
-
substrate of the protein kinases CSK and CHK, which specifically phosphorylate a tyrosine residue at the C-terminus forming intramolecular bonds to the SH2 domain and inhibiting the Src family kinase, overview
-
-
?
ATP + Src family kinase
ADP + phospho-L-tyrosinyl Src family kinase
-
terminal Src kinase Csk specifically phosphorylates Src family kinases on a C-terminal Tyr residue, which down-regulates their activities, identification of the docking determinants in Src recognized by the Csk substrate-docking site
-
-
?
ATP + Src protein
ADP + Src protein phosphate
MATK can phosphorylate the carboxyl-terminal conserved tyrosine of the Src protein
-
-
?
ATP + STAT3
ADP + phospho-L-tyrosinyl-STAT3
-
-
-
-
?
ATP + STAT3
ADP + phospho-tyrosinyl-STAT3
ATP + Tc10/Cdc42 GTPase-activating protein
ADP + phospho-L-tyrosinyl-Tc10/Cdc42 GTPase-activating protein
ATP + thyroid hormone receptor associated protein 3
?
-
-
-
-
?
ATP + TRK-fused gene
?
-
-
-
-
?
ATP + Tyr267 of Vav1
ADP + phosphorylated Tyr267 of Vav1
-
-
isoform c-Abl kinase probably regulates the activity of Rho guanine exchange factor Vav1 by direct phosphorylation at Tyr267 in the Dbl homology domain. The C-terminal SH3-SH2-SH3 domain and proline-rich region of Vav1 are required for its interaction with c-Abl kinase
-
?
ATP + zinc finger, CCHC domain containing protein 8
?
-
-
-
-
?
ATP + [Abi1]-L-tyrosine
ADP + [Abi1]-L-tyrosine phosphate
-
c-Abl phosphorylates Y213 of Abi1
-
-
?
ATP + [actin-stabilizing adapter protein HS1]-L-tyrosine
ADP + [actin-stabilizing adapter protein HS1]-L-tyrosine phosphate
-
c-Abl binds to phospho-HS1 via its SH2 domains and is required for full tyrosine phosphorylation of HS1 during T-cell activation
-
-
?
ATP + [androgen receptor]-L-tyrosine
ADP + [androgen receptor]-L-tyrosine phosphate
-
-
-
-
?
ATP + [aryl hydrocarbon receptor]-L-tyrosine
ADP + [aryl hydrocarbon receptor]-L-tyrosine phosphate
ATP + [c-Cbl]-L-tyrosine
ADP + [c-Cbl]-L-tyrosine phosphate
ATP + [carrier protein-intein-CAEEEIYGEFEA]-L-tyrosine
ADP + [carrier protein-intein-CAEEEIYGEFEA]-L-tyrosine phosphate
-
substrate is synthesized by fusing a 27 kDa carrier protein to intein which is linked to the peptide CAEEEIYGEFEA derived from human cyclin-dependent kinase harboring a phosphorylation site for Src kinase
-
-
?
ATP + [carrier protein-intein-CIGEGKYGVVYK]-L-tyrosine
ADP + [carrier protein-intein-CIGEGKYGVVYK]-L-tyrosine phosphate
-
substrate is synthesized by fusing a 27 kDa carrier protein to intein which is linked to the peptide CIGEGKYGVVYK derived from human cyclin-dependent kinase harboring a phosphorylation site for Src kinase
-
-
?
ATP + [carrier protein-intein-CIGEGTFGVVYK]-L-tyrosine
ADP + [carrier protein-intein-CIGEGTFGVVYK]-L-tyrosine phosphate
-
substrate is synthesized by fusing a 27 kDa carrier protein to intein which is linked to the peptide CIGEGTFGVVYK derived from human cyclin-dependent kinase harboring a phosphorylation site for Src kinase
-
-
?
ATP + [carrier protein-intein-CIGEGTpYGVVYK]-L-tyrosine
ADP + [carrier protein-intein-CIGEGTpYGVVYK]-L-tyrosine phosphate
-
substrate is synthesized by fusing a 27 kDa carrier protein to intein which is linked to the peptide CIGEGTpYGVVYK derived from human cyclin-dependent kinase harboring a phosphorylation site for Src kinase
-
-
?
ATP + [carrier protein-intein-CIGEGTYFVVYK]-L-tyrosine
ADP + [carrier protein-intein-CIGEGTYFVVYK]-L-tyrosine phosphate
-
substrate is synthesized by fusing a 27 kDa carrier protein to intein which is linked to the peptide CIGEGTYFVVYK derived from human cyclin-dependent kinase harboring a phosphorylation site for Src kinase
-
-
?
ATP + [carrier protein-intein-CIGEGTYGVEYK]-L-tyrosine
ADP + [carrier protein-intein-CIGEGTYGVEYK]-L-tyrosine phosphate
-
substrate is synthesized by fusing a 27 kDa carrier protein to intein which is linked to the peptide CIGEGTYGVEYK derived from human cyclin-dependent kinase harboring a phosphorylation site for Src kinase
-
-
?
ATP + [carrier protein-intein-CIGEGTYGVVFK]-L-tyrosine
ADP + [carrier protein-intein-CIGEGTYGVVFK]-L-tyrosine phosphate
-
substrate is synthesized by fusing a 27 kDa carrier protein to intein which is linked to the peptide CIGEGTYGVVFK derived from human cyclin-dependent kinase harboring a phosphorylation site for Src kinase
-
-
?
ATP + [carrier protein-intein-CIGEGTYGVVYK]-L-tyrosine
ADP + [carrier protein-intein-CIGEGTYGVVYK]-L-tyrosine phosphate
-
substrate is synthesized by fusing a 27 kDa carrier protein to intein which is linked to the peptide CIGEGTYGVVYK derived from human cyclin-dependent kinase harboring a phosphorylation site for Src kinase
-
-
?
ATP + [carrier protein-intein-CIGKGTYGVVYK]-L-tyrosine
ADP + [carrier protein-intein-CIGKGTYGVVYK]-L-tyrosine phosphate
-
substrate is synthesized by fusing a 27 kDa carrier protein to intein which is linked to the peptide CIGKGTYGVVYK derived from human cyclin-dependent kinase harboring a phosphorylation site for Src kinase
-
-
?
ATP + [disabled-1 adaptor protein]-L-tyrosine
ADP + [disabled-1 adaptor protein]-L-tyrosine phosphate
ATP + [estrogen receptor alpha]-L-tyrosine
ADP + [estrogen receptor alpha]-L-tyrosine phosphate
-
estrogen receptor alpha associates with c-Abl nonreceptor tyrosine kinase. The direct interaction is mediated by two PXXP motifs of estrogen receptor alpha and the c-Abl SH3 domain. Estrogen receptor alpha can be phosphorylated on residues Y52 and Y219. Phosphorylation by c-Abl stabilizes estrogen recptor alpha, resulting in enhanced estrogen receptor alpha transcriptional activity and increased expression of endogenous target genes. Phosphorylation at the Y219 site affects DNA binding and dimerization by estrogen receptor alpha. c-Abl kinase activity is required for regulation of the estrogen receptor alpha function, and a Y52F/Y219F mutant estrogen receptor leads to reduced breast cancer cell growth and invasion, estrogen receptor alpha associates with c-Abl nonreceptor tyrosine kinase. The direct interaction is mediated by two PXXP motifs of estrogen receptor alpha and the c-Abl SH3 domain. Estrogen receptor alpha can be phosphorylated on residues Y52 and Y219. Phosphorylation by c-Abl stabilizes estrogen receptor alpha, resulting in enhanced estrogen receptor alpha transcriptional activity and increased expression of endogenous target genes. Phosphorylation at the Y219 site affects DNA binding and dimerization by estrogen receptor alpha
-
?
ATP + [FAK]-L-tyrosine
ADP + [FAK]-L-tyrosine phosphate
ATP + [fibroblast growth factor receptor FGFR2]-L-tyrosine
ADP + [fibroblast growth factor receptor FGFR2]-L-tyrosine phosphate
ATP + [fibroblast growth factor receptor FGFR3]-L-tyrosine
ADP + [fibroblast growth factor receptor FGFR3]-L-tyrosine phosphate
ATP + [hyperpolarization-activated, cyclic nucleotide-gated 4 channel]-L-tyrosine
ADP + [hyperpolarization-activated, cyclic nucleotide-gated 4 channel]-L-tyrosine phosphate
ATP + [kdSrc kinase]-L-tyrosine
ADP + [kdSrc kinase]-L-tyrosine phosphate
ATP + [kinase Btk29]-L-tyrosine
ADP + [kinase Btk29]-L-tyrosine phosphate
-
-
-
-
?
ATP + [P-110]-L-tyrosine
ADP + [P-110]-L-tyrosine phosphate
-
-
-
-
?
ATP + [p110 catalytic subunit of PI 3-kinase]-L-tyrosine
ADP + [p110 catalytic subunit of PI 3-kinase]-L-tyrosine phosphate
-
-
-
-
?
ATP + [p21Cip1]-L-tyrosine
ADP + [p21Cip1]-L-tyrosine phosphate
-
-
-
-
?
ATP + [p27Kip1]-L-tyrosine
ADP + [p27Kip1]-L-tyrosine phosphate
-
-
-
-
?
ATP + [p57Kip2]-L-tyrosine
ADP + [p57Kip2]-L-tyrosine phosphate
-
-
-
-
?
ATP + [parkin]-Tyr143
ADP + [parkin]-phospho-Tyr143
-
-
nonreceptor tyrosine kinase c-Abl phosphorylates tyrosine 143 of parkin, which encodes a ubiquitin E3 ligase, related to autosomal recessive Parkinson disease. Phosphorylation inhibits parkin's ubiquitin E3 ligase activity and protective function
-
?
ATP + [protein kinase C zeta]-L-tyrosine
ADP + [protein kinase C zeta]-L-tyrosine phosphate
-
Src kinase plays an important role in angiotensin II-elicited protein kinase C zeta activation and the subsequent downstream signaling including ERK1/2 activation and vascular smooth muscle cell proliferation
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
ATP + [ring canal protein]-L-tyrosine
ADP + [ring canal protein]-L-tyrosine phosphate
-
-
-
-
?
ATP + [Runx1]-L-tyrosine
ADP + [Runx1]-L-tyrosine phosphate
ATP + [Sam68]-L-tyrosine
ADP + [Sam68]-L-tyrosine phosphate
ATP + [Signal Transducer and Activation of Transcription (STAT) protein]-L-tyrosine
ADP + [Signal Transducer and Activation of Transcription (STAT) protein]-L-tyrosine phosphate
-
-
-
?
ATP + [Src-family protein tyrosine kinase]-L-tyrosine
ADP + [Src-family protein tyrosine kinase]-L-tyrosine phosphate
-
i.e. SFK, substrate of protein tyrosine kinases Csk and Chk, phosphorylation at the regulatory tyrosine leading to inhibition of the SFK
-
-
?
ATP + [Stat5B]-L-tyrosine
ADP + [Stat5B]-L-tyrosine phosphate
-
activation by non-receptor tyrosine kinase Pyk2
-
-
?
ATP + [transmembrane adaptor protein LAT]-L-tyrosine
ADP + [transmembrane adaptor protein LAT]-L-tyrosine phosphate
-
substrate of ZAP-70
-
-
?
ATP + [tubulin]-L-tyrosine
ADP + [tubulin]-L-tyrosine phosphate
-
highly active with c-Fes, which also catalyzes tubulin polymerization in vitro
-
-
?
ATP + [vimentin]-L-tyrosine
ADP + [vimentin]-L-tyrosine phosphate
-
-
-
?
ATP + [ZAP-70]-L-tyrosine
ADP + [ZAP-70]-L-tyrosine phosphate
ATP + [[Lys19]Cdc2-(6-20) peptide]-L-tyrosine
?
-
i.e. KVEKIGEGTYGVVKK
-
-
?
denatured enolase + ATP
phosphorylated denatured enolase + ADP
-
-
-
?
gelsolin + ATP
phospho-tyrosinyl gelsolin + ADP
p130Cas + ATP
phospho-tyrosinyl p130Cas + ADP
-
phosphorylation of the Crk and Nck adaptor protein by Fak
-
-
?
paxillin + ATP
phospho-tyrosinyl paxillin + ADP
STAT transcription activator protein + ATP
phosphorylated STAT transcription activator protein + ADP
Wiskott-Aldrich syndrome protein + ATP
phospho-tyrosinyl Wiskott-Aldrich syndrome protein + ADP
-
i.e. WASP, phosphorylation by Fak
-
-
?
additional information
?
-
ATP + a protein
ADP + a phosphoprotein
autophosphorylation
-
-
?
ATP + a protein
ADP + a phosphoprotein
autophosphorylation
-
-
?
ATP + a protein
ADP + a phosphoprotein
phosphorylates tyrosine, serine and threonine
-
-
?
ATP + a protein
ADP + a phosphoprotein
the enzyme controls shoot and floral meristem size
-
-
?
ATP + a protein
ADP + a phosphoprotein
enzyme contributes to signal transduction
-
-
?
ATP + a protein
ADP + a phosphoprotein
enzyme is required in early larval development
-
-
?
ATP + a protein
ADP + a phosphoprotein
-
-
-
-
?
ATP + a protein
ADP + a phosphoprotein
-
PhK phosphorylates e.g. the protein substrate GPb, v-Fps phosphorylates e.g. the peptide substrate EAEIYEAEI, Csk phosphorylates e.g. the substrate poly-Glu4-Tyr
-
-
?
ATP + a protein
ADP + a phosphoprotein
it is likely that LIMK is involved in developmental or oncogenic processes through interactions with these LIM-containing proteins
-
-
?
ATP + a protein
ADP + a phosphoprotein
autophosphorylation
-
-
?
ATP + a protein
ADP + a phosphoprotein
autophosphorylation
-
-
?
ATP + a protein
ADP + a phosphoprotein
enzyme plays an important role in spermatogenesis
-
-
?
ATP + a protein
ADP + a phosphoprotein
ILK is a receptor-proximal protein kinase regulating integrin-mediated signal transduction
-
-
?
ATP + a protein
ADP + a phosphoprotein
enzyme is upregulated in HT-144 melanoma cells following TGF-beta1 stimulation
-
-
?
ATP + a protein
ADP + a phosphoprotein
ILK is involved in agonist stimulated, Pi(3)K-dependent, PKB/AKT activation. ILK is thus a receptor-proximal effector for the Pi(3)K-dependent, extracellular matrix and growth factor mediated, activation of PKB/AKT, and inhibition of GSK-3
-
-
?
ATP + a protein
ADP + a phosphoprotein
TESK1 has a specific function in spermatogenesis
-
-
?
ATP + a protein
ADP + a phosphoprotein
the enzyme induces formation of actin stress fibers and focal adhesions
-
-
?
ATP + a protein
ADP + a phosphoprotein
proximal mediators of IL-1 signaling
-
-
?
ATP + a protein
ADP + a phosphoprotein
apoptosis-inducing kinase
-
-
?
ATP + a protein
ADP + a phosphoprotein
NF-kappaB-activating and cell death-inducing kinase
-
-
?
ATP + a protein
ADP + a phosphoprotein
the enzyme is a downstream effector of activated Ras. Interaction with Ras leads to Raf-1 activation and results in transduction of cell growth and differentiation signals
-
-
?
ATP + a protein
ADP + a phosphoprotein
enzyme functions as an intermediary in TNFalpha-induced apoptosis
-
-
?
ATP + a protein
ADP + a phosphoprotein
enzyme plays a critical role in cell growth and development
-
-
?
ATP + a protein
ADP + a phosphoprotein
serine-threonine kinase
-
-
?
ATP + a protein
ADP + a phosphoprotein
role for this kinase in spermatogenesis
-
-
?
ATP + a protein
ADP + a phosphoprotein
TESK1 has a specific function in spermatogenesis
-
-
?
ATP + a protein
ADP + a phosphoprotein
the enzyme induces formation of actin stress fibers and focal adhesions
-
-
?
ATP + a protein
ADP + a phosphoprotein
-
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
-
660885, 661230, 661273, 661396, 661540, 663021, 702439, 703984, 703985, 704787, 705448, 705953, 706405, 706765, 706766, 737321, 737757, 738741, 739714 -
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
activation of Syk is responsible for K-Cl cotransport in SS cells by relieving Src-mediated inhibition of the transporter
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
enzymes of the Tec tyrosine kinase family phosphorylate themselves or other family members
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
substrate docking-site and binding structure of Src involving R279, R281, and R283
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
-
-
-
?
ATP + Abl
ADP + phospho-L-tyrosinyl-Abl
-
Abl is an important substrate for Src signalling in normal cells
-
-
?
ATP + Abl
ADP + phospho-L-tyrosinyl-Abl
-
Abl is a substrate of Src
-
-
?
ATP + Abl
ADP + phospho-L-tyrosinyl-Abl
-
Abl is an important substrate for Src signalling in normal cells, Abl is also required for Src-induced transformation of mouse fibroblasts, overview
-
-
?
ATP + Abl
ADP + phospho-L-tyrosinyl-Abl
-
Abl is a substrate of Src, phosphorylation on Tyr245 and Tyr412
-
-
?
ATP + Akt tyrosine kinase
ADP + phosphotyrosinyl-Akt
-
-
-
-
?
ATP + Akt tyrosine kinase
ADP + phosphotyrosinyl-Akt
-
tyrosine kinase Akt is phosphorylated by PYK2 for activation of the Akt signaling pathway, overview
-
-
?
ATP + Bad protein
ADP + phosphotyrosinyl Bad protein
-
substrate of Akt
-
-
?
ATP + Bad protein
ADP + phosphotyrosinyl Bad protein
-
substrate of Akt
-
-
?
ATP + beta-catenin
ADP + phospho-tyrosinyl-beta-catenin
-
-
-
-
?
ATP + beta-catenin
ADP + phospho-tyrosinyl-beta-catenin
-
-
-
-
?
ATP + beta-catenin
ADP + phospho-tyrosinyl-beta-catenin
-
-
-
-
?
ATP + Cas protein
ADP + phospho-tyrosinyl-Cas protein
-
-
-
-
?
ATP + Cas protein
ADP + phospho-tyrosinyl-Cas protein
-
-
-
-
?
ATP + Cas protein
ADP + phospho-tyrosinyl-Cas protein
-
-
-
-
?
ATP + cdc2
ADP + phosphorylated cdc2
-
-
-
?
ATP + cdc2
ADP + phosphorylated cdc2
the Cdc2-inhibitory kinase is required for preventing premature activation of the mitotic program. Maternally provided Dwee1 is sufficient for regulating Cdc2 during embryogenesis
-
-
?
ATP + cdc2
ADP + phosphorylated cdc2
phosphorylated exclusively on Y15
-
?
ATP + cofilin
ADP + phosphorylated cofilin
phosphorylation specifically at Ser-3
-
-
?
ATP + cofilin
ADP + phosphorylated cofilin
phosphorylation specifically at Ser-3
-
-
?
ATP + cortactin
ADP + phospho-tyrosinyl-cortactin
-
-
-
-
?
ATP + cortactin
ADP + phospho-tyrosinyl-cortactin
-
-
-
-
?
ATP + cortactin
ADP + phospho-tyrosinyl-cortactin
-
-
-
-
?
ATP + cyclin-associated cyclin-dependent kinase
ADP + phosphorylated cyclin-associated cyclin-dependent kinase
phosphorylated on Y15
-
?
ATP + cyclin-associated cyclin-dependent kinase
ADP + phosphorylated cyclin-associated cyclin-dependent kinase
Wee1 negatively regulates cyclin-dependent kinases by phosphorylation on Y15
-
?
ATP + epidermal growth factor receptor
ADP + phospho-L-tyrosinyl-epidermal growth factor receptor
-
the activated Abl tyrosine kinase negaively regulates endocytosis of the epidermal growth factor, e.g. in NR6 cells, overview, Abl allows the ligand-activated EGFR to escape Cbl-dependent down-regulation by inhibiting the accumulation of Cbl at the plasma membrane in response to epidermal growth factor stimulation and disrupting the formation of the EGFR-Cbl complex without affecting Cbl protein stability
-
-
?
ATP + epidermal growth factor receptor
ADP + phospho-L-tyrosinyl-epidermal growth factor receptor
-
activated Abl phosphorylates the EGFR primarily on Tyr1173, no activity with the Tyr1173 mutant substrate
-
-
?
ATP + ezrin
ADP + phospho-tyrosinyl-ezrin
-
-
-
-
?
ATP + ezrin
ADP + phospho-tyrosinyl-ezrin
-
-
-
-
?
ATP + ezrin
ADP + phospho-tyrosinyl-ezrin
-
-
-
-
?
ATP + FAK
ADP + phospho-tyrosinyl-FAK
-
-
-
-
?
ATP + FAK
ADP + phospho-tyrosinyl-FAK
-
-
-
-
?
ATP + FAK
ADP + phospho-tyrosinyl-FAK
-
-
-
-
?
ATP + glycogen synthase kinase 3beta
ADP + phosphotyrosinyl glycogen synthase kinase 3beta
-
substrate of Akt
-
-
?
ATP + glycogen synthase kinase 3beta
ADP + phosphotyrosinyl glycogen synthase kinase 3beta
-
substrate of Akt
-
-
?
ATP + IkappaBalpha-L-tyrosine
ADP + IkappaBalpha-L-tyrosine phosphate
-
p56lck regulates cell motility and nuclear factor kappaB-mediated secretion of urokinase type plasminogen activator through tyrosine phosphorylation of IkappaBalpha following hypoxia/reoxygenation, molecular mechanism, physiological role
-
-
?
ATP + IkappaBalpha-L-tyrosine
ADP + IkappaBalpha-L-tyrosine phosphate
-
Lck interacts via its SH2 domain with tyrosine-phosphorylated IkappaBalpha
-
-
?
ATP + myelin basic protein
ADP + phosphorylated myelin basic protein
serine/threonine kinase activity
-
-
?
ATP + myelin basic protein
ADP + phosphorylated myelin basic protein
serine/threonine-specific kinase activity
-
-
?
ATP + p120 protein
ADP + phospho-tyrosinyl-p120 protein
-
-
-
-
?
ATP + p120 protein
ADP + phospho-tyrosinyl-p120 protein
-
-
-
-
?
ATP + p120 protein
ADP + phospho-tyrosinyl-p120 protein
-
-
-
-
?
ATP + p190 GTPase
ADP + phospho-tyrosinyl-p190 GTPase
-
-
-
-
?
ATP + p190 GTPase
ADP + phospho-tyrosinyl-p190 GTPase
-
-
-
-
?
ATP + p190 GTPase
ADP + phospho-tyrosinyl-p190 GTPase
-
-
-
-
?
ATP + p32-L-tyrosine
ADP + p32-L-tyrosine phosphate
-
-
-
-
?
ATP + p32-L-tyrosine
ADP + p32-L-tyrosine phosphate
-
p32 is a sperm protein
-
-
?
ATP + p34cdc2
ADP + phosphorylated p34cdc2
phosphorylated exclusively on Y15
-
-
?
ATP + p34cdc2
ADP + phosphorylated p34cdc2
Wee1 kinase inhibits mitosis by directly phosphorylating p34cdc2 on Y15
-
?
ATP + PAK1
ADP + phospho-L-tyrosinyl-PAK1
-
Jak2 is involved in the regulation of serine-threonine kinase PAK1, maximal cell motility is required for tyrosyl phosphorylation of PAK1
-
-
?
ATP + PAK1
ADP + phospho-L-tyrosinyl-PAK1
-
a serine-threonine kinase, phosphorylation at Y153, Y201, and Y285 activates PAK1, no activation of PAK1 mutants Y153F,Y201F,Y285F, mutational analysis of phosphorylation sites,overview
-
-
?
ATP + paxillin
ADP + phospho-tyrosinyl-Shc paxillin
-
-
-
-
?
ATP + paxillin
ADP + phospho-tyrosinyl-Shc paxillin
-
-
-
-
?
ATP + paxillin
ADP + phospho-tyrosinyl-Shc paxillin
-
-
-
-
?
ATP + PIKE-A
ADP + phosphotyrosinyl-PIKE-A
-
i.e. phosphatidylinositol 3-kinase enhancer-activating Akt, phosphorylation by fyn is essential for PIKE-A complex formation and apoptotic cleavage, overview
-
-
?
ATP + PIKE-A
ADP + phosphotyrosinyl-PIKE-A
-
i.e. phosphatidylinositol 3-kinase enhancer-activating Akt, phosphorylation at Y682 and Y774 by fyn, the kinase domain of activated fyn binds to the ArfGAP domain of PIKE-A, reduced activity with Y682F and with Y774F mutant PIKE-A, no activity with Y682F/Y774F mutant PIKE-A
-
-
?
ATP + plakoglobin
ADP + phospho-tyrosinyl-plakoglobin
-
-
-
-
?
ATP + plakoglobin
ADP + phospho-tyrosinyl-plakoglobin
-
-
-
-
?
ATP + plakoglobin
ADP + phospho-tyrosinyl-plakoglobin
-
-
-
-
?
ATP + poly(Glu4-Tyr)
ADP + poly(Glu4-Tyr)-L-tyrosine phosphate
-
-
-
-
?
ATP + poly(Glu4-Tyr)
ADP + poly(Glu4-Tyr)-L-tyrosine phosphate
-
-
-
?
ATP + poly(Glu4-Tyr)
ADP + poly(Glu4-Tyr)-L-tyrosine phosphate
-
artificial substrate
-
-
?
ATP + protein
ADP + protein tyrosine phosphate
phosphorylates the regulatory C-terminal tyrosine residue present on cytoplasmic tyrosine kinases of the Src family
-
-
?
ATP + protein
ADP + protein tyrosine phosphate
CSK phosphorylates other members of the src-family of tyrosine kinases at their regulatory carboxy-terminus
-
-
?
ATP + protein tyrosine
ADP + protein tyrosine phosphate
protein kinase activity with specificity for tyrosine residues
-
-
?
ATP + protein tyrosine
ADP + protein tyrosine phosphate
p135tyk2 tyrosine kinase directly binds and tyrosine phosphorylates alpha subunit of the type I IFN receptor, IFN-R
-
-
?
ATP + protein tyrosine
ADP + protein tyrosine phosphate
specifically phosphorylates Tyr527 of p60c-src from neonatal rat brain, specifically phosphorylates a negative regulatory site of p60c-src
-
-
?
ATP + Rho protein
ADP + phospho-tyrosinyl-Rho protein
-
-
-
-
?
ATP + Rho protein
ADP + phospho-tyrosinyl-Rho protein
-
-
-
-
?
ATP + Rho protein
ADP + phospho-tyrosinyl-Rho protein
-
-
-
-
?
ATP + Shc protein
ADP + phospho-tyrosinyl-Shc protein
-
-
-
-
?
ATP + Shc protein
ADP + phospho-tyrosinyl-Shc protein
-
-
-
-
?
ATP + Shc protein
ADP + phospho-tyrosinyl-Shc protein
-
-
-
-
?
ATP + signal transducer and activator of transcription
ADP + phospho-L-tyrosinyl-signal transducer and activator of transcription
-
-
-
-
?
ATP + signal transducer and activator of transcription
ADP + phospho-L-tyrosinyl-signal transducer and activator of transcription
-
-
-
-
?
ATP + STAT3
ADP + phospho-tyrosinyl-STAT3
-
-
-
-
?
ATP + STAT3
ADP + phospho-tyrosinyl-STAT3
-
-
-
-
?
ATP + STAT3
ADP + phospho-tyrosinyl-STAT3
-
-
-
-
?
ATP + Tc10/Cdc42 GTPase-activating protein
ADP + phospho-L-tyrosinyl-Tc10/Cdc42 GTPase-activating protein
-
physical and functional interaction of Fyn with the brain-enriched Rho GTPase-activating protein Tc10/Cdc42 GTPase-activating protein, i.e. TCGAP, TCGAP is involved in Fyn-mediated regulation of axon and dendrite outgrowth
-
-
?
ATP + Tc10/Cdc42 GTPase-activating protein
ADP + phospho-L-tyrosinyl-Tc10/Cdc42 GTPase-activating protein
-
physical and functional interaction of Fyn with the brain-enriched Rho GTPase-activating protein Tc10/Cdc42 GTPase-activating protein, i.e. TCGAP, phosphorylation mainly at Tyr406, no activity with TCGAP Y406F mutant, recombinant substrate from mouse and human, overview
-
-
?
ATP + [aryl hydrocarbon receptor]-L-tyrosine
ADP + [aryl hydrocarbon receptor]-L-tyrosine phosphate
-
Src tyrosine kinases are involved in a signaling transduction pathway activating aryl hydrocarbon receptor AhR-mediated signalling by omeprazole or 2,3,7,8-tetrachlorodibenzo-4-dioxin TCDD ligand-binding, AhR phosphorylation at Tyr320, the omeprazole-dependent mechanism probably involves S318 and K316
-
-
?
ATP + [aryl hydrocarbon receptor]-L-tyrosine
ADP + [aryl hydrocarbon receptor]-L-tyrosine phosphate
-
in vivo assay utilizing Hep-G2 cells or H4IIE cells expressing AhR and Src kinase
-
-
?
ATP + [c-Cbl]-L-tyrosine
ADP + [c-Cbl]-L-tyrosine phosphate
-
proto-oncogenic PTK protein substrate
-
-
?
ATP + [c-Cbl]-L-tyrosine
ADP + [c-Cbl]-L-tyrosine phosphate
-
activity and phosphorylation patterns of Syk, Fyn, and Abl with recombinant wild-type and mutant Y700F, Y731F, and Y774F c-Cbl proteins, phosphorylation site preferences are determined by interaction of the enzymes' SH2 domain with the substrate via p85, a phosphatidylinositol 3-kinase, overview
-
-
?
ATP + [disabled-1 adaptor protein]-L-tyrosine
ADP + [disabled-1 adaptor protein]-L-tyrosine phosphate
-
-
-
-
?
ATP + [disabled-1 adaptor protein]-L-tyrosine
ADP + [disabled-1 adaptor protein]-L-tyrosine phosphate
-
activation of disabled-1 adaptor protein Dab1, which is responsible for regulation of neuronal migrations during mammalian brain development, Reelin induces tyrosine-phosphorylated-Dab1 degradation and downregulates Dab1 expression in primary cortical neurons, mutant non-phosphorylated Dab1 are not degraded, pathway regulation, overview
-
-
?
ATP + [disabled-1 adaptor protein]-L-tyrosine
ADP + [disabled-1 adaptor protein]-L-tyrosine phosphate
-
-
-
-
?
ATP + [disabled-1 adaptor protein]-L-tyrosine
ADP + [disabled-1 adaptor protein]-L-tyrosine phosphate
-
activation of disabled-1 adaptor protein Dab1, which is responsible for regulation of neuronal migrations during mammalian brain development, Reelin induces tyrosine-phosphorylated-Dab1 degradation and downregulates Dab1 expression in primary cortical neurons, mutant non-phosphorylated Dab1 are not degraded, pathway regulation, overview
-
-
?
ATP + [FAK]-L-tyrosine
ADP + [FAK]-L-tyrosine phosphate
-
-
-
?
ATP + [FAK]-L-tyrosine
ADP + [FAK]-L-tyrosine phosphate
activation of FAK during epiboly and gastrulation by dynamic phosphorylation at Tyr861
-
-
?
ATP + [fibroblast growth factor receptor FGFR2]-L-tyrosine
ADP + [fibroblast growth factor receptor FGFR2]-L-tyrosine phosphate
-
activation by non-receptor tyrosine kinase Pyk2, interaction via the FGFR juxtamembrane and the Pyk2 kinase domain, activation is antagonized by tyrosine phosphatase Shp2
-
-
?
ATP + [fibroblast growth factor receptor FGFR2]-L-tyrosine
ADP + [fibroblast growth factor receptor FGFR2]-L-tyrosine phosphate
-
activation by non-receptor tyrosine kinase Pyk2, interaction via the FGFR juxtamembrane and the Pyk2 kinase domain
-
-
?
ATP + [fibroblast growth factor receptor FGFR3]-L-tyrosine
ADP + [fibroblast growth factor receptor FGFR3]-L-tyrosine phosphate
-
activation by non-receptor tyrosine kinase Pyk2, interaction via the FGFR juxtamembrane and the Pyk2 kinase domain, activation is antagonized by tyrosine phosphatase Shp2
-
-
?
ATP + [fibroblast growth factor receptor FGFR3]-L-tyrosine
ADP + [fibroblast growth factor receptor FGFR3]-L-tyrosine phosphate
-
activation by non-receptor tyrosine kinase Pyk2, interaction via the FGFR juxtamembrane and the Pyk2 kinase domain
-
-
?
ATP + [hyperpolarization-activated, cyclic nucleotide-gated 4 channel]-L-tyrosine
ADP + [hyperpolarization-activated, cyclic nucleotide-gated 4 channel]-L-tyrosine phosphate
substrate HCN4, tyrosine 531 is phosphorylated
-
-
?
ATP + [hyperpolarization-activated, cyclic nucleotide-gated 4 channel]-L-tyrosine
ADP + [hyperpolarization-activated, cyclic nucleotide-gated 4 channel]-L-tyrosine phosphate
-
substrate HCN4, tyrosine 531 is phosphorylated
-
-
?
ATP + [kdSrc kinase]-L-tyrosine
ADP + [kdSrc kinase]-L-tyrosine phosphate
-
i.e. kinase-defective chicken Src mutant K295M
-
-
?
ATP + [kdSrc kinase]-L-tyrosine
ADP + [kdSrc kinase]-L-tyrosine phosphate
-
i.e. kinase-defective Src, substrate of Chk and Csk, inactivation mechanism of Src, overview
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
-
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
-
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
-
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
-
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
-
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
-
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
-
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
-
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
-
-
-
?
ATP + [Runx1]-L-tyrosine
ADP + [Runx1]-L-tyrosine phosphate
-
-
-
?
ATP + [Runx1]-L-tyrosine
ADP + [Runx1]-L-tyrosine phosphate
the enzyme phosphorylates transcription factor Runx1 and regulates Runx1-mediated megakaryocyte maturation
-
-
?
ATP + [Sam68]-L-tyrosine
ADP + [Sam68]-L-tyrosine phosphate
-
-
-
?
ATP + [Sam68]-L-tyrosine
ADP + [Sam68]-L-tyrosine phosphate
-
-
-
?
ATP + [Sam68]-L-tyrosine
ADP + [Sam68]-L-tyrosine phosphate
SRMS regulates the phosphorylation of Sam68 in an EGF-dependent manner in MDA-MB 231 cells
-
-
?
ATP + [Sam68]-L-tyrosine
ADP + [Sam68]-L-tyrosine phosphate
the enzyme (SRMS) regulates the phosphorylation of Sam68 in an EGF-dependent manner in MDA-MB 231 cells
-
-
?
ATP + [Sam68]-L-tyrosine
ADP + [Sam68]-L-tyrosine phosphate
phosphoproteomics analysis identifies novel candidate substrates of the enzyme (SRMS)
-
-
?
ATP + [ZAP-70]-L-tyrosine
ADP + [ZAP-70]-L-tyrosine phosphate
-
substrate of Lck, Fyn, and c-Abl, leads to ZAP-70 activation, mechanism
-
-
?
ATP + [ZAP-70]-L-tyrosine
ADP + [ZAP-70]-L-tyrosine phosphate
-
substrate of Lck, Fyn, and c-Abl
-
-
?
gelsolin + ATP
phospho-tyrosinyl gelsolin + ADP
-
phosphorylation by PYK2 increases the binding of gelsolin to phosphoatidylinositol lipids and actin polymerization at the fibroblastic cell periphery
-
-
?
gelsolin + ATP
phospho-tyrosinyl gelsolin + ADP
-
phosphorylation by PYK2
-
-
?
paxillin + ATP
phospho-tyrosinyl paxillin + ADP
-
phosphorylation at Tyr31 and Tyr118 by Fak plays a role in tumor cell motility inhibition
-
-
?
paxillin + ATP
phospho-tyrosinyl paxillin + ADP
-
phosphorylation at Tyr31 and Tyr118 by Fak
-
-
?
STAT transcription activator protein + ATP
phosphorylated STAT transcription activator protein + ADP
-
activation of STAT by phosphorylation is required for translocation to the nucleus, the enzyme regulates the cytokine expression via STAT, overview
-
-
?
STAT transcription activator protein + ATP
phosphorylated STAT transcription activator protein + ADP
-
phosphorylation by Jak2 at tyrosine residues
-
-
?
STAT transcription activator protein + ATP
phosphorylated STAT transcription activator protein + ADP
-
activation of STAT by phosphorylation is required for translocation to the nucleus, the enzyme regulates the cytokine expression via STAT, overview
-
-
?
STAT transcription activator protein + ATP
phosphorylated STAT transcription activator protein + ADP
-
phosphorylation by Jak2 at tyrosine residues
-
-
?
STAT transcription activator protein + ATP
phosphorylated STAT transcription activator protein + ADP
-
activation of STAT by phosphorylation is required for translocation to the nucleus, the enzyme regulates the cytokine expression via STAT, overview
-
-
?
STAT transcription activator protein + ATP
phosphorylated STAT transcription activator protein + ADP
-
phosphorylation by Jak2 at tyrosine residues
-
-
?
additional information
?
-
oncogene v-fps induces fibrosarcomas in birds
-
-
?
additional information
?
-
-
oncogene v-fps induces fibrosarcomas in birds
-
-
?
additional information
?
-
oncogene v-fps induces fibrosarcomas in birds
-
-
?
additional information
?
-
enzyme can have a protein-protein interaction, through its putative SH3 binding site, with at least two intracellular SH3-containing proteins
-
-
?
additional information
?
-
-
enzyme can have a protein-protein interaction, through its putative SH3 binding site, with at least two intracellular SH3-containing proteins
-
-
?
additional information
?
-
the receptor controls dauer larva development
-
-
?
additional information
?
-
enzyme is involved in TGFbeta signaling
-
-
?
additional information
?
-
cell-surface receptor required for transduction of environmental signals into an appropriate developmental response, controls dauer larva development
-
-
?
additional information
?
-
-
IP3 production in the hypersensitive response of lemon seedlings against Alternaria alternata involves active protein tyrosine kinases but not a G-protein, overview
-
-
?
additional information
?
-
Yes kinase is required during development, overview
-
-
?
additional information
?
-
-
Yes kinase is required during development, overview
-
-
?
additional information
?
-
the Yes kinase performs autophosphorylation
-
-
?
additional information
?
-
-
the Yes kinase performs autophosphorylation
-
-
?
additional information
?
-
-
-
-
?
additional information
?
-
-
-
-
-
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in vitro autophosphorylation activity at tyrosine residues
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in vitro autophosphorylation activity at tyrosine residues
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required maternally for the establishment of the normal array of embryonic segments
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additional information
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plays important roles in cell adhesion, functions downstream of integrins, enzyme is involved in integrin-mediated cell adhesion signaling
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additional information
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plays important roles in cell adhesion, functions downstream of integrins, enzyme is involved in integrin-mediated cell adhesion signaling
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additional information
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mutations in the gene encoding the Drosophila tyrosine kinase Abelson substantially enhanced the severity of the CNS phenotype of armadillo mutations, consistent with these proteins functioning co-operatively at adherens junctions in both the CNS and the epidermis
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additional information
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Jak2 is involved in transcriptional signaling and ligand-independent gene expression, and increases the activity of erythropoietin receptor cell-surface expression, overview, enzyme deficiency is involved in lymphoid leukemia, overview
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additional information
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receptor-bound Jak2 allows the transphosphorylation of the dimeric receptor molecule one another
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additional information
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Etk is essential for polymyxin resistance, while Wzc is not
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additional information
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protein kinases and protein phosphatases regulate enzyme activities in the cell, overview
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poor activity on free amino acids, consensus sequence of c-Src is E-EIYE/G-XF, that of v-Fps is E-IYE-XI/V, and that of Csk is IYM-F-F-F, specificity overview
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Wee1: substrate specificity
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catalytic domain Src including the C-terminal tail autophosphorylates and efficiently phosphorylates substrate peptides and proteins. Autophosphorylation occurs by an intermolecular mechanism
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p60src, the transforming protein of Rous sarcoma virus, is a protein kinase that has a strict specificity for Tyr. The phosphorylation of cellular proteins by p60src results in transformation
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transforms NIH 3T3 cells
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enzyme plays a critical role in a variety of signal transduction pathways
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enzyme plays a critical role in a variety of signal transduction pathways
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additional information
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Src and Src-family protein-tyrosine kinases are proto-oncogenes important in cell morphology, motility, proliferation, and survival, regulation by reversible phosphorylation, overview
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JAK2 plays a central role in non-protein tyrosine kinase receptor signaling pathways
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JAK2 plays a central role in non-protein tyrosine kinase receptor signaling pathways
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interaction of the Fyn SH3 domain with the p85 subunit of PI3-kinase
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activates NF-kappaB
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PTK6 may function as an intracellular signal transducer in specific tissues
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PTK6 may function as an intracellular signal transducer in specific tissues
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transcriptionally induced in normal T cells by interleukin 2 stimulation, roles in T cell proliferation and differentiation
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sensitizes mammary epithelial cells to epidermal growth factor
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sensitizes mammary epithelial cells to epidermal growth factor
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involved in signal transduction by association with a number of membrane receptors
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enzyme may serve specialized functions in hemopoietic cells, it is possible that damage to HCK may contribute to the pathogenesis of some human leukemias
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enzyme may serve specialized functions in hemopoietic cells, it is possible that damage to HCK may contribute to the pathogenesis of some human leukemias
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Hck is involved in a number of cell signal transduction pathways, frequently in pathways associated with immune response
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Hck is involved in a number of cell signal transduction pathways, frequently in pathways associated with immune response
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participates in signal transduction events regulating the growth, differentiation and function of phagocytes
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additional information
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it may be involved in key regulatory processes
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p135tyk2 tyrosine kinase directly binds and tyrosine phosphorylates alpha subunit of the type I IFN receptor, IFN-R. Tyk2 protein functions as part of a receptor complex to initiate intracellular signaling in response to type I interferons
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p135tyk2 tyrosine kinase directly binds and tyrosine phosphorylates alpha subunit of the type I IFN receptor, IFN-R. Tyk2 protein functions as part of a receptor complex to initiate intracellular signaling in response to type I interferons
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ZAP-70 that associates with T cell antigen receptor zeta chain and undergoes tyrosine phosphorylation following TCR stimulation
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tandem ZAP-70 SH2 domains bind phosphorylated, but not nonphosphorylated, T cell antigen receptor zeta cyt. The NH2-terminal ZAP-70 SH2 domain also binds to T cell antigen receptor zeta cyt but with 100-fold lower affinity. No binding is observed with the COOH-terminal ZAP-70 SH2 domain. Similar studies demonstrate that the ZAP-70 tandem SH2 domain can bind a T cell antigen receptor zeta 3 TAM peptide in which both tyrosine residues are phosphorylated: Little or no binding is observed with peptides phosphorylated at only one tyrosine residue, or a nonphosphorylated peptide. Binding of the tandem SH2 domains to the other two TCR zeta TAM peptides and to a CD3 epsilon TAM peptide is also observed. All four doubly tyrosine phosphorylated TAM peptides cross-compete with each other for binding to the tandem SH2 domains of ZAP-70. The affinity of these peptides for the tandem SH2 construct demonstrates a hierarchy of TAM zeta 1, TAM zeta 2, TAM epsilon, TAM zeta 3
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?
additional information
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mutations of Jak-3 gene in patients with autosomal severe combined immune deficiency
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JAK3 deficiency in a patient with severe combined immunodeficiency over 20 years after bone marrow transplantation: persistence of genetically and biochemically defective autologous B cells, associated with reconstitution of cellular and humoral immunity, suggests that integrity of the gammac-JAK3 signalling pathway is not strictly required for immunoglobulin production
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JAK3 deficiency in humans results in autosomal recessive T-B+ severe combined immunodeficiency disease
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HYL plays a significant role in the signal transduction of hematopoietic cells
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HYL plays a significant role in the signal transduction of hematopoietic cells
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enzyme plays a pivotal role in cell signal transduction
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may play an important role in thymopoiesis, role in controlling cellular growth and differentiation
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may play an important role in thymopoiesis, role in controlling cellular growth and differentiation
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effector of phosphatidylinositol 3'-kinase and is involved in interleukin 6-induced neuroendocrine differentiation of prostate cancer cells
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additional information
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autosomal recessive form of severe combined immunodeficiency disease in which ZAP-70 is absent as a result of mutations in the ZAP-70 gene. This absence is associated with defects in TCR signal transduction. Integral role in T cell activation and differentiation
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may play a role in the growth and differentiation of hematopoietic cells
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additional information
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may play a role in the growth and differentiation of hematopoietic cells
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may have a role in human cancer
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JAK3 splice isoforms are functional in JAK3 signaling and may enrich the complexity of the intracellular response functional in IL-2 or cytokine signaling
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additional information
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mutations of the Janus family kinase JAK3 are responsible for autosomal recessive severe combined immunodeficiency. Abnormalities in tyrosine phosphorylation of JAK3 in response to interleukin-2 (IL-2) and IL-4 is present in all patients. In one patient carrying a single amino acid change, Glu481Gly, in the JH3 domain of JAK3, a partially conserved IL-2 responses is observed resulting in reduced but detectable levels of JAK3 and STAT5 phosphorylation. A single cysteine to arginine substitution, Cys759Arg, results in high basal levels of constitutive JAK3 tyrosine phosphorylation unresponsive to either downregulation by serum starvation or cytokine-mediated upregulation
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additional information
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mutations of the Janus family kinase JAK3 are responsible for autosomal recessive severe combined immunodeficiency. Abnormalities in tyrosine phosphorylation of JAK3 in response to interleukin-2 (IL-2) and IL-4 is present in all patients. In one patient carrying a single amino acid change, Glu481Gly, in the JH3 domain of JAK3, a partially conserved IL-2 responses is observed resulting in reduced but detectable levels of JAK3 and STAT5 phosphorylation. A single cysteine to arginine substitution, Cys759Arg, results in high basal levels of constitutive JAK3 tyrosine phosphorylation unresponsive to either downregulation by serum starvation or cytokine-mediated upregulation
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additional information
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the receptor shares two-hit inactivation mechanism with tumor suppressor genes and mutation of it may occur in the early stage of tumorgenesis
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mutations in the activin receptor-like kinase 1 gene in hereditary haemorrhagic telangiectasia type 2
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activin and its receptor play an important role in development
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the activin receptor-like kinase 1 gene is the second locus for the autosomal dominant vascular disease hereditary hemorrhagic telangiectasia
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signal transduction by TGF bet involves the formation of a heteromeric complex of two different serine/threonine kinase receptors
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?
additional information
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insensitivity to anti-mullerian hormone is due to a mutation in the human anti-mullerian hormone receptor
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?
additional information
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transforming growth factor-beta regulates cell cycle progression by a unique signaling mechanism that involves its binding to the type II TGF beta receptor and activation of type I
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?
additional information
?
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transforming growth factor-beta regulates cell cycle progression by a unique signaling mechanism that involves its binding to the type II TGF beta receptor and activation of type I
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?
additional information
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enzyme is involved in bone morphogenetic protein signaling
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enzyme is involved in bone morphogenetic protein signaling
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RIP2 interacts with members of the TNFR-1 signaling complex, including inhibitor of apoptosis protein cIAP1 and with members of the TNFR-associated factor family, specifically TRAF1, TRAF5, and TRAF6, but not with TRAF2, TRAF3, or TRAF4
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?
additional information
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CARDIAK may be involved in NF-kappa B/JNK signaling and in the generation of the proinflammatory cytokine IL-1 beta through activation of caspase-1
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?
additional information
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blocks cell division when overexpressed in Hela cells
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activity of WEE1Hu is regulated by phosphorylation and proteolytic degradation, WEE1Hu plays a role in inhibiting mitosis before M phase by phosphorylating cyclin B1-Cdc2
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?
additional information
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activity of WEE1Hu is regulated by phosphorylation and proteolytic degradation, WEE1Hu plays a role in inhibiting mitosis before M phase by phosphorylating cyclin B1-Cdc2
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?
additional information
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active c-Fes tyrosine kinase binds tubulin and microtubules through separate domains and promotes microtubule assembly, c-Fes colocalization with microtubules in vivo requires the SH2 enzyme domain, implication in the differentiation of vascular, endothelial, myeloid, hematopoietic, and neuronal cells, overview
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additional information
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ALK-MYH9 performs tyrosine autophosphorylation in vivo, but not in vitro, possible mechanism
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additional information
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Fes tyrosine kinase promotes survival and terminal granulocyte differentiation of factor-dependent myeloid progenitors (32D) and activates lineage-specific transcription factors, e.g. CCAAT/enhancer-binding protein-alpha and STAT3, down-regulation of macrophage marker F4/80
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additional information
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JAK2 is an important intracellular mediator of cytokine signalling, JAK2 deficiency may lead to hematologic cancers, and a number of immune diseases
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additional information
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protein tyrosine kinases are involved in downstream signaling pathways, e.g. BCR/ABL kinase in the phosphatidylinositol 3'-kinase pathway, required for regulation of cell differentiation and cell cycle regulation, BCR/ABL and several other constitutive protein tyrosine kinases are activated in myeloid malignancies, overview, protein deregulation probable due to fusion gene formation because of chromosomal translocations or as distinct gain-of-function point mutations, autophosphorylation of BCR/ABL kinase at Tyr177 is essential for myeloid leukomogenesis in vivo, expression of BCR/ABL kinase leads to functional downregulation of the basal transcription factor TFIIH involved in nucleotide excision DNA repair pathway, and to activation of RAD51 also involved in DNA repair, overview
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additional information
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protein tyrosine kinases play a critical role in the modulation of a wide range of cellular events such as cell division, cell differentiation, and cell metabolism, over-stimulation of PTKs impairs normal cell growth, resulting in oncogenic transformation, regulation of enzyme activity occurs in dynamic oscillatory behaviour, patterns and mechanism, overview
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additional information
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PTKs are involved in cell signalling
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additional information
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spleen tyrosine kinase Syk modulates epidermal growth factor receptor EGFR signalling in mammary epithelial cells acting as a negative controle element, regulation of EGFR by activation of the autophosphorylation activity of EGFR, but not of HER2 and HER3, overview
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?
additional information
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Src and Src-family protein-tyrosine kinases are proto-oncogenes important in cell morphology, motility, proliferation, and survival, regulation by reversible phosphorylation, overview
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?
additional information
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Src-dependent outside-in signalling is a key step in the process of autoregulation of beta2 integrins in polymorphonuclear cells and required for adhesion of interleukin-8, Src PTKs are required for macrophage antigen-1-mediated adhesion, which is inhibited by cytochalasin D and involved F-actin and protein P-110, overview
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?
additional information
?
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Src-family protein tyrosine kinases are proto-oncogenic enzymes controlling mammalian cell growth and proliferation, the enzymes are regulated by activation through autophosphorylation of their kinase domain and by inhibition through phosphorylation of their regulatory tyrosine residue near the C-terminus, mechanism, overview, abberrant SFK activation contributes to cancer development
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additional information
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Syk kinase is involved in cell motility and activation of phosphatidylinositol 3'-kinase, Syk kinase inhibits the tyrosine phosphorylation of IkappaBalpha and thus inhibits activation of NFkappaB via interaction of IkappaBalpha and phosphatidylinositol 3'-kinase, pathway regulation, overview
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additional information
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Tec family tyrosine kinases play a central role in hematopoietic cellular signaling
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additional information
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the enzyme is regulated in balance with protein tyrosine phosphatase, complex regulation mechanism, overview, the enzyme has decreasing effect, opposing to receptor protein tyrosine kinase EGFR, on volume-sensitive chloride current in atrial myocytes, overview
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?
additional information
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the Fes tyrosine kinase is regulated via its SH2 domain
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additional information
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the Janus kinase is involved in the JAK-STAT signaling cascade causing inflammatory activity in the brain
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additional information
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the Src tyrosine kinase regulates and stimulates silica particle formation in lung epithelium which induces interleukin-8 release activating the signaling cascade via phosphorylation of MAPK and ERK, overview
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?
additional information
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the Syk family tyrosine kinase ZAP-70 is required to couple the activated T-cell antigen receptor TCR to downstream signaling pathways, binding of TCR via its SH2 domains, regulation mechanism, overview
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additional information
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c-Fes interacts with soluble unpolymerized tubulin via its N-terminal Fes/CIP4 homology FCH domain
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additional information
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Csk-substrate interaction requires the SH2 and SH3 enzyme domains
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additional information
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low tyrosine autophosphorylation activities of chimeric Alk-NPM and ALK-TPM3
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additional information
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Pyk2 performs autophosphorylation at Tyr402, fibroblast growth factor receptors FGFR1 and FGFR4 are no substrates of Pyk2
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?
additional information
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site specificity of tyrosine phosphorylation by Tec family members, overview
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additional information
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Syk kinase performs autophosphorylation
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additional information
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Syk performs autophosphorylation
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additional information
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the activation loop is not essential for enzyme activity
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additional information
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the BCR/ABL kinase performs tyrosine autophosphorylation, mechanism
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additional information
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a multisite model for Fyn binding and regulation, overview, subtype-selective modulation by tyrosine phosphorylation/dephosphorylation provides a mechanism for differential regulation of sodium channels by neurotrophins and tyrosine phosphorylation in unmyelinated axons and dendrites, where NaV1.2 channels are expressed in brain neurons, overview
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?
additional information
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Brutons tyrosine kinase is involved in B lymphocyte chemotaxis and homing, overview
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additional information
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c-Abl activates p21 transcription via interaction with and regulation of the DNA-binding of p53, c-Abl also recruits p53 to the p21 promoter, overview
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additional information
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c-Abl is regulated by conformational changes through intramolecular interactions and phosphorylation, overview
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additional information
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c-Src is a physiologically relevant substrate for Methionine aminopeptidases, whose dysfunction is likely to account for the cell-cycle effects of MetAP inhibitors including bengamide A, overview
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?
additional information
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dynamics of BCR-ABL kinase domain mutations in chronic myeloid leukemia after sequential treatment with multiple tyrosine kinase inhibitors, overview
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?
additional information
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dynamics of BCR-ABL kinase domain mutations in chronic myeloid leukemia after sequential treatment with multiple tyrosine kinase inhibitors, overview
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additional information
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enzyme deficiency leads to X-linked agammaglobulinemia, XLA, a humoral primary immunodeficiency in which affected patients have very low levels of peripheral B cells and a profound deficiency of all immunoglobulin isotypes, overview
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additional information
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enzyme deficiency leads to X-linked agammaglobulinemia, XLA, a humoral primary immunodeficiency in which affected patients have very low levels of peripheral B cells and a profound deficiency of all immunoglobulin isotypes, overview
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additional information
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FAK plays a role in the anoikis phenomenon or anchorage-dependent cell survival, and in angiogenesis and formation of new blood vessels, overview, downstream targets of the FAK and PYK2 are MAP kinases implicated in proliferative processes, PYK2 is an essential linker between G-protein coupled receptor and the MAPK cascade, overview
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additional information
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Fes is involved in the regulation of cell-cell and cell-matrix interactions mediated by adherens junctions and focal adhesions, the activated form of the kinase can induce cellular transformation, overview
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?
additional information
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Fyn tyrosine kinase is involved in actin stress fiber formation in fibroblasts
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additional information
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Jak2 is involved in transcriptional signaling and ligand-independent gene expression, and increases the activity of erythropoietin receptor cell-surface expression, overview, enzyme deficiency is involved in lymphoid leukemia, overview
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?
additional information
?
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p38 MAP kinase inhibitor SB203580 and protein tyrosine kinase inhibitor tyrphostin 25 combined can be used for inhibition of matrix metalloproteinase-9 expression, overview
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?
additional information
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protein-tyrosine kinase Syk plays a central role in Fcgamma receptor-mediated phagocytosis in the adaptive immune system, and is required for pathogen engulfment in complement-mediated phagocytosis
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?
additional information
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Src and Abl regulation, overview, cytoplasmic tyrosine kinase Src is involved in signal transduction induced by growth factors and integrins, Src also shows oncogenic activity when it is deregulated, Abl mediates Src-induced extracellular regulated kinase 5, ERK5, activation to drive cell transformation, Abl/Rac and Abl/ERK5 pathways also operate in human MCF7 and BT549 breast cancer cells, where neoplastic transformation depends on Src-like activities, overview
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additional information
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Src PTK plays a role in NF-kappaB activation in epithelial cells, Src PTKs are important in regulation of vascular permeability and acute inflammatory responses, and are essential for the recruitment and activation of monocytes, macrophages, neutrophils, and other immune cells, Src PTKs can also regulate the functional activity of these receptors and is involved in cell signaling, biological functions, cellular and molecular mechanisms, overview
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?
additional information
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Syk protein tyrosine kinase is involved in lipopolysaccharide-induced responses and intracellular signaling leading to release of pro-inflammatory mediators in macrophages, overview
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?
additional information
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the BCR-ABL tyrosine kinase is inhibited in Philadelphia chromosome-positive chronic myeloid leukemia, CML, overview
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?
additional information
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the enzyme tyrosine phosphorylates a wide range of proteins, especially nuclear matrix proteins
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additional information
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the Src family of protein kinases mediates mitogenic signal transduction, and constitutive activation of the enzymes is associated with tumorigenesis
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additional information
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the Src protein tyrosine kinase p56Lck plays a critical role in the O2 sensitivity of Kv1.3 channels and in signalling during hypoxia in T lymphocytes, overview
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additional information
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the Src-family tyrosine kinase fyn phosphorylates phosphatidylinositol 3-kinase enhancer-activating Akt, preventing its apoptotic cleavage and promoting cell survival, overview
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?
additional information
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Toll-like receptors TLR-8 and TLR-9 require activation/phosphorylation by Btk for acting incell signaling, overview, enzyme deficiency is involved in development of male immune disorder X-linked agammaglobulineamia, XLA
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additional information
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tyrosine kinase Src is a key enzyme in mammalian signal transduction and an important target for anticancer drug discovery
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additional information
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tyrosine kinases play a fundamental role in cell proliferation, survival, adhesion, and motility and have also been shown to mediate malignant cell transformation, Brk may play a key role in lymphomagenesis
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additional information
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Abl does not mediate tyrosine phosphorylation of Stat3 and Shc, two important regulators of Src oncogenic activity
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additional information
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Btk can interact with the TIR domains of Toll-like receptors TLR-8 and TLR-9
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additional information
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BTK performs autophosphorylation
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additional information
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Btk performs autophosphorylation on Tyr223
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additional information
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c-Abl performs autophosphorylation
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additional information
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FAk binds interaction partners, e.g. paxillin, talin, and p190RhoGEF, at the FAT domain, i.e. the focal adhesion targeting domain, at the C-terminal domain modulating the Fak activity, overview
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?
additional information
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receptor-bound Jak2 allows the transphosphorylation of the dimeric receptor molecule one another
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?
additional information
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Src PTKs phosphorylate substrates in the cytosol or at the inner face of the plasma membrane, e.g. Shc, Rho GTPase-activating protein p190, and transcription factor STAT3, substrates at cell-matrix adhesions, e.g. cytoskeleton-associated proteins such as focal adhesion kinase FAK, Cas, paxillin, ezrin, and cortactin, and substrates at cell-cell adhesions, e.g. junctional proteins such as beta-catenin, p120, and plakoglobin
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additional information
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Syk affects actin dynamics around the C3bi-mediated phagosomes
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additional information
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the enzyme is activated by phosphorylation, and also performs autophosphorylation
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additional information
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the enzyme performs autophosphorylation at tyrosine residues
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additional information
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after platelet stimulation, integrin alphaIIbbeta3 binds to the enzyme's SH3 domain at a site overlapping with its PPII helix binding site
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?
additional information
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p40mos binds ATP analog p-fluorosulfonylbenzoyladenosine and exhibits ATPase activity
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?
additional information
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p40mos binds ATP analog p-fluorosulfonylbenzoyladenosine and exhibits ATPase activity
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?
additional information
?
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p40mos binds ATP analog p-fluorosulfonylbenzoyladenosine and exhibits ATPase activity
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-
?
additional information
?
-
all isoforms of the activin receptor type II bind inhibin A with low affinity
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?
additional information
?
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the bone morphogenetic protein receptor binds bone morphogenetic protein 2 and bone morphogenetic protein 4
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-
?
additional information
?
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the bone morphogenetic protein receptor binds bone morphogenetic protein 2 and bone morphogenetic protein 4
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-
?
additional information
?
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the bone morphogenetic protein receptor binds bone morphogenetic protein 2 and bone morphogenetic protein 4
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-
?
additional information
?
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activates NF-kappaB
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-
?
additional information
?
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-
activates NF-kappaB
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-
?
additional information
?
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role for JAK3 in hematopoiesis and T- and B-cell development
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-
?
additional information
?
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involvement of the Jak-3 Janus kinase in signalling by interleukins 2 and 4 in lymphoid and myeloid cells
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-
?
additional information
?
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JAK3 kinase is associated with terminal differentiation of hematopoietic cells
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?
additional information
?
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the enzyme transduces signals initiated by integrin engagement and G protein-coupled receptors. Several splice isoforms of FAK are preferentially expressed in rat brain, some of which have an increased autophosphorylation activity
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?
additional information
?
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activation of FadK may be an important early step in intracellular signal transduction pathways triggered in response to cell interactions with the extracellular matrix
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-
?
additional information
?
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activation of FadK may be an important early step in intracellular signal transduction pathways triggered in response to cell interactions with the extracellular matrix
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-
?
additional information
?
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lskT-encoded protein-tyrosine kinase may aid in transducing proliferative or differentiative signals unique to lymphocytes
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-
?
additional information
?
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lskT-encoded protein-tyrosine kinase may aid in transducing proliferative or differentiative signals unique to lymphocytes
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?
additional information
?
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enzyme is implicated in neoplastic transformation
-
-
?
additional information
?
-
-
enzyme is implicated in neoplastic transformation
-
-
?
additional information
?
-
enzyme is involved in pathway for signaling through glycosyl-phosphatidylinositol (GPI)-anchored membrane proteins
-
-
?
additional information
?
-
elevated levels of p56tck can contribute to the malignant properties of LSTRA cells
-
-
?
additional information
?
-
-
elevated levels of p56tck can contribute to the malignant properties of LSTRA cells
-
-
?
additional information
?
-
p56lck can positively regulate T-cell functions and it mediates at least some of the effects of CD4 and CD8 on T-cell activation
-
-
?
additional information
?
-
-
p56lck can positively regulate T-cell functions and it mediates at least some of the effects of CD4 and CD8 on T-cell activation
-
-
?
additional information
?
-
p56lck participates in lymphocyte-specific signal transduction pathways. Disturbances in lck expression may contribute to the pathogenesis of some human neoplastic diseases
-
-
?
additional information
?
-
-
p56lck participates in lymphocyte-specific signal transduction pathways. Disturbances in lck expression may contribute to the pathogenesis of some human neoplastic diseases
-
-
?
additional information
?
-
may be specifically involved in the cell growth of hepatocytes or in the step of hepatocarcinogenesis
-
-
?
additional information
?
-
-
may be specifically involved in the cell growth of hepatocytes or in the step of hepatocarcinogenesis
-
-
?
additional information
?
-
may interact with the intracellular domain of cell surface receptors
-
-
?
additional information
?
-
participates in the signalling pathways of a broad range of cytokines
-
-
?
additional information
?
-
-
participates in the signalling pathways of a broad range of cytokines
-
-
?
additional information
?
-
enzyme is crucial for B cell development. Loss of kinase activity results in the human immunodeficiency, X-linked agammaglobulinemia, characterized by a failure to produce B cells
-
-
?
additional information
?
-
-
enzyme is crucial for B cell development. Loss of kinase activity results in the human immunodeficiency, X-linked agammaglobulinemia, characterized by a failure to produce B cells
-
-
?
additional information
?
-
directly implicated in the pathogenesis of X-linked agammaglobulinaemia
-
-
?
additional information
?
-
-
directly implicated in the pathogenesis of X-linked agammaglobulinaemia
-
-
?
additional information
?
-
deficient expression of a B cell cytoplasmic tyrosine kinase in human X-linked agammaglobulinemia
-
-
?
additional information
?
-
perinatal lethality and blocked B-cell development in mice lacking the tyrosine kinase Syk. Syk-deficient radiation chimaeras fail to accumulate mature B cells, Syk-deficient mice show impaired development of thymocytes using the V gamma 3 variable region gene, Syk is not required for signalling through the IL-2 and G-CSF receptors
-
-
?
additional information
?
-
Rlk has potential functions in intrathymic T cell development and mature T cell signaling
-
-
?
additional information
?
-
Ntk may play an inhibitory role in the control of T-cell proliferation
-
-
?
additional information
?
-
role for JAK1 kinase in the differentiation or function of a subset of CNS neurons
-
-
?
additional information
?
-
-
role for JAK1 kinase in the differentiation or function of a subset of CNS neurons
-
-
?
additional information
?
-
activating motif occurs in four discrete steps: binding of p59fyn, phosphorylation of the motif, binding of ZAP-70, and activation of ZAP-70 kinase activity
-
-
?
additional information
?
-
Ctk is involved in the regulation of neural function and differentiation of male germ cells through interactions with members of the Src family kinases
-
-
?
additional information
?
-
could be responsible for the tyrosine phosphorylation observed in a murine thymic medullary epithelial cell line E-5 following complex formation with thymocytes
-
-
?
additional information
?
-
type II receptor isoforma exist which play preferential binding to TGF-beta2 and have their own defined role in debvelopment
-
-
?
additional information
?
-
mRIP3 uses a novel mechanism to induce death
-
-
?
additional information
?
-
-
mRIP3 uses a novel mechanism to induce death
-
-
?
additional information
?
-
in a cell cycle the wee1 kinase is phosphorylated at M-phase, phosphorylation occurs in the N-terminal domain resulting in inactivation of the kinase activity. The N-terminal domain, or the entire molecule is extensively phosphorylated by cdc2-cyclin B kinase
-
-
?
additional information
?
-
-
CX3CL1, i.e. fractalkine, only member of the delta subclass of chemokines, triggers PTK Syk activity in monocytes/macrophages localized in F-actin-enriched cell protrusions, which are formed due to CX3CL1 treatment and subsequent increase in F-actin, Syk deficiency results in strong impairment of RAW cell migration to CX3CL1, overview
-
-
?
additional information
?
-
-
Fps/Fes and Fer protein-tyrosine kinases play redundant roles in regulating hematopoiesis
-
-
?
additional information
?
-
-
Fps/Fes tyrosine kinase is involved in regulation of erythropoiesis and of myeloid differentiation and survival
-
-
?
additional information
?
-
-
protein tyrosine kinases are involved in downstream signaling pathways, e.g. BCR/ABL kinase in the phosphatidylinositol 3'-kinase pathway, required for regulation of cell differentiation and cell cycle regulation, expression of BCR/ABL kinase leads to functional downregulation of the basal transcription factor TFIIH involved in nucleotide excision DNA repair pathway, and to activation of RAD51 also involved in DNA repair, overview
-
-
?
additional information
?
-
-
Src family kinases Hck, Fyn and Src are constitutively expressed and are required for murine embryonic stem cell growth and differentiation, regulation of SFKs in response to leukemia inhibitory factor LIF and other growth factors, overview
-
-
?
additional information
?
-
-
the enzyme plays an important role in the self-renewal and as comitogen in the movement of stem cells out of the haematopoietic stem cell pool into the progeny pool, regulation of bone marrow cell migration
-
-
?
additional information
?
-
-
the BCR/ABL kinase performs tyrosine autophosphorylation, mechanism
-
-
?
additional information
?
-
-
Brutons tyrosine kinase is involved in B lymphocyte chemotaxis and homing, overview
-
-
?
additional information
?
-
-
Csk is essential for mouse embryonic development, Csk plays a role in G protein-coupled receptor- and receptor tyrosine kinase-induced fibroblast cell migration, overview, modeling of Csk regulation of focal adhesion turnover
-
-
?
additional information
?
-
-
enzyme-deficient endothelial cells shows reduced migration, as well as decreased cell proliferation and survival in vivo
-
-
?
additional information
?
-
-
Jak2 is involved in transcriptional signaling and ligand-independent gene expression, and increases the activity of erythropoietin receptor cell-surface expression, overview, enzyme deficiency is involved in lymphoid leukemia, overview
-
-
?
additional information
?
-
-
PYK2 is involved in vascular endothelial growth factor-induced activities, such as cell migration, blood vessel formation, Pyk2 forms complexes with Src tyrosine kinase for activation of the Akt tyrosine kinase pathway, PYK2 is required in receptor- and ischemia-activated signaling events leading to endothelial NO synthase phosphorylation and modulation of endothelial NO synthase-mediated vasoactive function and angiogenic response, PYK2 is involved in Ca2+ mobilization in muscle cells, overview
-
-
?
additional information
?
-
-
spleen tyrosine kinase Syk is necessary for E-selectin-induced alpha(L)beta(2) integrin-mediated rolling on intercellular adhesion molecule-1, neutrophil activation pathways, overview
-
-
?
additional information
?
-
-
Src and Abl regulation, overview, cytoplasmic tyrosine kinase Src is involved in signal transduction induced by growth factors and integrins, Src also shows oncogenic activity when it is deregulated, Abl mediates Src-induced extracellular regulated kinase 5, ERK5, activation to drive cell transformation
-
-
?
additional information
?
-
-
Src PTK plays a role in NF-kappaB activation in epithelial cells, Src PTKs are important in regulation of vascular permeability and acute inflammatory responses, and are essential for the recruitment and activation of monocytes, macrophages, neutrophils, and other immune cells, Src PTKs can also regulate the functional activity of these receptors and is involved in cell signaling, biological functions, cellular and molecular mechanisms, overview
-
-
?
additional information
?
-
-
the Brutons tyrosine kinase is a critical signaling mediator downstream of the B cell Ag receptor, plays a role in regulating TLR-induced cytokine production, and is required for TLR-induced IL-10 production in multiple macrophage populations and in TLR signaling, overview, X-linked agammaglobulinemia is caused by mutations in Btk resulting in multiple defects in B cell development and function, and recurrent bacterial infections, Btk-dependent induction of NFkappaB and AP-1 DNA binding activity
-
-
?
additional information
?
-
the enzyme is involved in cytokine signaling
-
-
?
additional information
?
-
-
the enzyme is involved in cytokine signaling
-
-
?
additional information
?
-
-
tyrosine kinase Fyn determines the specific localization of TrkB brain-derived neurotrophic factor, BDNF, receptor to intracellular lipid rafts in cortical and hippocampal membranes, this process is critically dependent on the tyrosine kinase Fyn, overview, role for lipid rafts in neurotrophin signaling
-
-
?
additional information
?
-
-
Abl does not mediate tyrosine phosphorylation of Stat3 and Shc, two important regulators of Src oncogenic activity
-
-
?
additional information
?
-
-
Fak binds interaction partners, e.g. paxillin, talin, and p190RhoGEF, at the FAT domain, i.e. the focal adhesion targeting domain, at the C-terminal domain modulaing the Fak activity, overview
-
-
?
additional information
?
-
-
receptor-bound Jak2 allows the transphosphorylation of the dimeric receptor molecule one another
-
-
?
additional information
?
-
-
Src PTKs phosphorylate substrates in the cytosol or at the inner face of the plasma membrane, e.g. Shc, Rho GTPase-activating protein p190, and transcription factor STAT3, substrates at cell-matrix adhesions, e.g. cytoskeleton-associated proteins such as focal adhesion kinase FAK, Cas, paxillin, ezrin, and cortactin, and substrates at cell-cell adhesions, e.g. junctional proteins such as beta-catenin, p120, and plakoglobin
-
-
?
additional information
?
-
-
the Brutons tyrosine kinase is a critical signaling mediator downstream of the B cell Ag receptor, plays a role in regulating TLR-induced cytokine production, and is required for TLR-induced IL-10 production in multiple macrophage populations and in TLR signaling, overview, X-linked agammaglobulinemia is caused by mutations in Btk resulting in multiple defects in B cell development and function, and recurrent bacterial infections, Btk-dependent induction of NFkappaB and AP-1 DNA binding activity
-
-
?
additional information
?
-
-
enzyme is involved in cell growth, differentiation, and apoptosis
-
-
?
additional information
?
-
-
antagonistic regulation of swelling-activated Cl- current in rabbit ventricle by Src and EGFR protein tyrosine kinases, overview
-
-
?
additional information
?
-
-
Src activates an outwardly rectifying chloride current in myocytes being involved in osmotic swelling, enzyme inhibition also inhibits stretch-activated Cl- current, mechanism, overview
-
-
?
additional information
?
-
-
Lyn is an important B cell signaling kinase of the Src tyrosine kinase family with a broad range of functions from cytoskeletal changes to induction of apoptosis, Lyn and and its interaction with rafts and TLR2 are involved in the initial stages of Pseudomonas aeruginosa interaction with host cells and invasion of an alveolar epithelial cell line, primary lung cells, and rat lungs by Pseudomonas aeruginosa, overview
-
-
?
additional information
?
-
specifically phosphorylates Tyr527 of p60c-src from neonatal rat brain. Specifically phosphorylates a negative regulatory site of p60c-src
-
-
?
additional information
?
-
CSK is involved in regulation of src family kinases
-
-
?
additional information
?
-
Batk may function as a brain-specific regulator of kinases involved in the development and maintenance of the nervous system
-
-
?
additional information
?
-
appear to play a role in B-cell-IgM and FcERI receptor signaling
-
-
?
additional information
?
-
TGF-beta RII expression is down-regulated in cells treated with exogenous TGF-beta1
-
-
?
additional information
?
-
mullerian inhibiting substance causes regression of the fetal Mullerian duct on binding a heteromeric complex of types I and II cell-surface receptors in the fetal urogenital ridge. The anti-mullerian hormone type II receptor provides specificity for mullerian inhibiting substance
-
-
?
additional information
?
-
-
protein tyrosine kinase-dependent modulation of voltage-dependent potassium channels by genistein in cardiac ventricular myocytes
-
-
?
additional information
?
-
-
the Src tyrosine kinase regulates and stimulates silica particle formation in epithelium which induces chemokine KIP-2 release activating the signaling cascade via phosphorylation of MAPK and ERK, overview
-
-
?
additional information
?
-
-
Src PTK plays a role in NF-kappaB activation in epithelial cells, Src PTKs are important in regulation of vascular permeability and acute inflammatory responses, and are essential for the recruitment and activation of monocytes, macrophages, neutrophils, and other immune cells, Src PTKs can also regulate the functional activity of these receptors and is involved in cell signaling, biological functions, cellular and molecular mechanisms, overview
-
-
?
additional information
?
-
-
Syk protein tyrosine kinase is involved in lipopolysaccharide-induced responses and intracellular signaling leading to release of pro-inflammatory mediators in macrophages, overview
-
-
?
additional information
?
-
-
tyrosine kinase Fyn determines the specific localization of TrkB brain-derived neurotrophic factor, BDNF, receptor in to intracellular lipid rafts in cortical and hippocampal membranes, this process is critically dependent on the tyrosine kinase Fyn, overview, role for lipid rafts in neurotrophin signaling
-
-
?
additional information
?
-
-
Src PTKs phosphorylate substrates in the cytosol or at the inner face of the plasma membrane, e.g. Shc, Rho GTPase-activating protein p190, and transcription factor STAT3, substrates at cell-matrix adhesions, e.g. cytoskeleton-associated proteins such as focal adhesion kinase FAK, Cas, paxillin, ezrin, and cortactin, and substrates at cell-cell adhesions, e.g. junctional proteins such as beta-catenin, p120, and plakoglobin
-
-
?
additional information
?
-
associated with breast cancer and osteoporosis
-
-
?
additional information
?
-
-
Src and Src-family protein-tyrosine kinases are proto-oncogenes important in cell morphology, motility, proliferation, and survival, regulation by reversible phosphorylation, overview
-
-
?
additional information
?
-
-
SH2 domain-based tyrosine kinase assay using biotin ligase modified with a terbium(III) complex. An SH2 domain from lymphocyte-specific tyrosine kinase is genetically fused to a truncated biotin carboxyl carrier protein, and the resulting fusion protein is labeled through biotinylation with biotin protein ligase carrying multiple copies of a luminescent Tb3+ complex. The labeled SH2 fusion proteins are employed to detect a phosphorylated peptide immobilized on the surface of the microtiter plate, where the phosphorylated peptide is produced by phosphorylation to the substrate peptide by Src tyrosine kinase. The assay allows for a reliable determination of the activity of Src kinase lower than 10 ng/mL
-
-
?
additional information
?
-
-
the enzyme is involved in regulation of sperm capacitation, signal transduction mechanism, capacitation mechanism, overview
-
-
?
additional information
?
-
is likely to participate in a variety of integrin-extracellular-matrix-dependent signaling events during morphogenesis
-
-
?
additional information
?
-
-
is likely to participate in a variety of integrin-extracellular-matrix-dependent signaling events during morphogenesis
-
-
?
additional information
?
-
participate in signalling pathways activated in response to cell interaction, role for FAK in gastrulation
-
-
?
additional information
?
-
-
participate in signalling pathways activated in response to cell interaction, role for FAK in gastrulation
-
-
?
additional information
?
-
yes gene product is likely to play an important role in oogenesis or early development
-
-
?
additional information
?
-
functions during reinitiation of meiotic division
-
-
?
additional information
?
-
the kinase induces progression through the cell cycle for both meiotic and mitotic cells
-
-
?
additional information
?
-
involved in signal transduction
-
-
?
additional information
?
-
importance of the function of activin receptor in the regulatory mechanism for body axis formation
-
-
?
additional information
?
-
down-regulation of Wee1-like kinase activity by phosphorylation at mitosis is a multistep process that occurs after other biochemical reactions have signaled the successful completion of S phase
-
-
?
additional information
?
-
possible function during secondary steps of tumor progression
-
-
?
additional information
?
-
possible function during secondary steps of tumor progression
-
-
?
additional information
?
-
-
possible function during secondary steps of tumor progression
-
-
?
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
ATP + a protein
ADP + a phosphoprotein
ATP + a [homeodomain-interacting protein kinase 2]-L-tyrosine
ADP + a [homeodomain-interacting protein kinase 2]-L-tyrosine phosphate
-
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
ATP + Abl
ADP + phospho-L-tyrosinyl-Abl
ATP + Akt tyrosine kinase
ADP + phosphotyrosinyl-Akt
-
tyrosine kinase Akt is phosphorylated by PYK2 for activation of the Akt signaling pathway, overview
-
-
?
ATP + Bad protein
ADP + phosphotyrosinyl Bad protein
ATP + beta-catenin
ADP + phospho-tyrosinyl-beta-catenin
ATP + Cas protein
ADP + phospho-tyrosinyl-Cas protein
ATP + cdc2
ADP + phosphorylated cdc2
the Cdc2-inhibitory kinase is required for preventing premature activation of the mitotic program. Maternally provided Dwee1 is sufficient for regulating Cdc2 during embryogenesis
-
-
?
ATP + cortactin
ADP + phospho-tyrosinyl-cortactin
ATP + cyclin-associated cyclin-dependent kinase
ADP + phosphorylated cyclin-associated cyclin-dependent kinase
Wee1 negatively regulates cyclin-dependent kinases by phosphorylation on Y15
-
?
ATP + epidermal growth factor receptor
ADP + phospho-L-tyrosinyl-epidermal growth factor receptor
-
the activated Abl tyrosine kinase negaively regulates endocytosis of the epidermal growth factor, e.g. in NR6 cells, overview, Abl allows the ligand-activated EGFR to escape Cbl-dependent down-regulation by inhibiting the accumulation of Cbl at the plasma membrane in response to epidermal growth factor stimulation and disrupting the formation of the EGFR-Cbl complex without affecting Cbl protein stability
-
-
?
ATP + ezrin
ADP + phospho-tyrosinyl-ezrin
ATP + FAK
ADP + phospho-tyrosinyl-FAK
ATP + glycogen synthase kinase 3beta
ADP + phosphotyrosinyl glycogen synthase kinase 3beta
ATP + IkappaBalpha-L-tyrosine
ADP + IkappaBalpha-L-tyrosine phosphate
-
p56lck regulates cell motility and nuclear factor kappaB-mediated secretion of urokinase type plasminogen activator through tyrosine phosphorylation of IkappaBalpha following hypoxia/reoxygenation, molecular mechanism, physiological role
-
-
?
ATP + NaV1.2 channel
ADP + phospho-L-tyrosinyl-NaV1.2 channel
-
Y66 and Y1893, which are in consensus sequences appropriate for binding to the Fyn SH2 domain after phosphorylation, are both required for optimal binding and regulation by Fyn. Y730, which is located near the SH3-binding motif in LI-II, and Y1497 and Y1498 in the inactivation gate in LIII-IV, are also required for optimal regulation, but phosphorylation of these sites likely promotes fast inactivation
-
-
?
ATP + p120 protein
ADP + phospho-tyrosinyl-p120 protein
ATP + p190 GTPase
ADP + phospho-tyrosinyl-p190 GTPase
ATP + p32-L-tyrosine
ADP + p32-L-tyrosine phosphate
-
-
-
-
?
ATP + p34cdc2
ADP + phosphorylated p34cdc2
Wee1 kinase inhibits mitosis by directly phosphorylating p34cdc2 on Y15
-
?
ATP + PAK1
ADP + phospho-L-tyrosinyl-PAK1
-
Jak2 is involved in the regulation of serine-threonine kinase PAK1, maximal cell motility is required for tyrosyl phosphorylation of PAK1
-
-
?
ATP + paxillin
ADP + phospho-tyrosinyl-Shc paxillin
ATP + PIKE-A
ADP + phosphotyrosinyl-PIKE-A
-
i.e. phosphatidylinositol 3-kinase enhancer-activating Akt, phosphorylation by fyn is essential for PIKE-A complex formation and apoptotic cleavage, overview
-
-
?
ATP + plakoglobin
ADP + phospho-tyrosinyl-plakoglobin
ATP + protein
?
CSK phosphorylates other members of the src-family of tyrosine kinases at their regulatory carboxy-terminus. By regulating the activity of these kinases, CSK may play an important role in cell growth and development
-
-
?
ATP + protein
ADP + protein tyrosine phosphate
ATP + protein tyrosine
ADP + protein tyrosine phosphate
ATP + protein tyrosine kinase Yes
ADP + phospho-L-tyrosinyl Yes
-
Csk inactivates the enzyme substrate
-
-
?
ATP + Rho protein
ADP + phospho-tyrosinyl-Rho protein
ATP + Shc protein
ADP + phospho-tyrosinyl-Shc protein
ATP + Src family kinase
?
-
substrate of the protein kinases CSK and CHK, which specifically phosphorylate a tyrosine residue at the C-terminus forming intramolecular bonds to the SH2 domain and inhibiting the Src family kinase, overview
-
-
?
ATP + Src family kinase
ADP + phospho-L-tyrosinyl Src family kinase
-
terminal Src kinase Csk specifically phosphorylates Src family kinases on a C-terminal Tyr residue, which down-regulates their activities, identification of the docking determinants in Src recognized by the Csk substrate-docking site
-
-
?
ATP + Src protein
ADP + Src protein phosphate
MATK can phosphorylate the carboxyl-terminal conserved tyrosine of the Src protein
-
-
?
ATP + STAT3
ADP + phospho-tyrosinyl-STAT3
ATP + Tc10/Cdc42 GTPase-activating protein
ADP + phospho-L-tyrosinyl-Tc10/Cdc42 GTPase-activating protein
-
physical and functional interaction of Fyn with the brain-enriched Rho GTPase-activating protein Tc10/Cdc42 GTPase-activating protein, i.e. TCGAP, TCGAP is involved in Fyn-mediated regulation of axon and dendrite outgrowth
-
-
?
ATP + [androgen receptor]-L-tyrosine
ADP + [androgen receptor]-L-tyrosine phosphate
-
-
-
-
?
ATP + [aryl hydrocarbon receptor]-L-tyrosine
ADP + [aryl hydrocarbon receptor]-L-tyrosine phosphate
-
Src tyrosine kinases are involved in a signaling transduction pathway activating aryl hydrocarbon receptor AhR-mediated signalling by omeprazole or 2,3,7,8-tetrachlorodibenzo-4-dioxin TCDD ligand-binding, AhR phosphorylation at Tyr320, the omeprazole-dependent mechanism probably involves S318 and K316
-
-
?
ATP + [c-Cbl]-L-tyrosine
ADP + [c-Cbl]-L-tyrosine phosphate
-
proto-oncogenic PTK protein substrate
-
-
?
ATP + [disabled-1 adaptor protein]-L-tyrosine
ADP + [disabled-1 adaptor protein]-L-tyrosine phosphate
ATP + [estrogen receptor alpha]-L-tyrosine
ADP + [estrogen receptor alpha]-L-tyrosine phosphate
-
estrogen receptor alpha associates with c-Abl nonreceptor tyrosine kinase. The direct interaction is mediated by two PXXP motifs of estrogen receptor alpha and the c-Abl SH3 domain. Estrogen receptor alpha can be phosphorylated on residues Y52 and Y219. Phosphorylation by c-Abl stabilizes estrogen recptor alpha, resulting in enhanced estrogen receptor alpha transcriptional activity and increased expression of endogenous target genes. Phosphorylation at the Y219 site affects DNA binding and dimerization by estrogen receptor alpha. c-Abl kinase activity is required for regulation of the estrogen receptor alpha function, and a Y52F/Y219F mutant estrogen receptor leads to reduced breast cancer cell growth and invasion
-
?
ATP + [FAK]-L-tyrosine
ADP + [FAK]-L-tyrosine phosphate
activation of FAK during epiboly and gastrulation by dynamic phosphorylation at Tyr861
-
-
?
ATP + [fibroblast growth factor receptor FGFR2]-L-tyrosine
ADP + [fibroblast growth factor receptor FGFR2]-L-tyrosine phosphate
-
activation by non-receptor tyrosine kinase Pyk2, interaction via the FGFR juxtamembrane and the Pyk2 kinase domain, activation is antagonized by tyrosine phosphatase Shp2
-
-
?
ATP + [fibroblast growth factor receptor FGFR3]-L-tyrosine
ADP + [fibroblast growth factor receptor FGFR3]-L-tyrosine phosphate
-
activation by non-receptor tyrosine kinase Pyk2, interaction via the FGFR juxtamembrane and the Pyk2 kinase domain, activation is antagonized by tyrosine phosphatase Shp2
-
-
?
ATP + [kinase Btk29]-L-tyrosine
ADP + [kinase Btk29]-L-tyrosine phosphate
-
-
-
-
?
ATP + [P-110]-L-tyrosine
ADP + [P-110]-L-tyrosine phosphate
-
-
-
-
?
ATP + [p110 catalytic subunit of PI 3-kinase]-L-tyrosine
ADP + [p110 catalytic subunit of PI 3-kinase]-L-tyrosine phosphate
-
-
-
-
?
ATP + [p21Cip1]-L-tyrosine
ADP + [p21Cip1]-L-tyrosine phosphate
-
-
-
-
?
ATP + [p27Kip1]-L-tyrosine
ADP + [p27Kip1]-L-tyrosine phosphate
-
-
-
-
?
ATP + [p57Kip2]-L-tyrosine
ADP + [p57Kip2]-L-tyrosine phosphate
-
-
-
-
?
ATP + [parkin]-Tyr143
ADP + [parkin]-phospho-Tyr143
-
-
nonreceptor tyrosine kinase c-Abl phosphorylates tyrosine 143 of parkin, which encodes a ubiquitin E3 ligase, related to autosomal recessive Parkinson disease. Phosphorylation inhibits parkin's ubiquitin E3 ligase activity and protective function
-
?
ATP + [protein kinase C zeta]-L-tyrosine
ADP + [protein kinase C zeta]-L-tyrosine phosphate
-
Src kinase plays an important role in angiotensin II-elicited protein kinase C zeta activation and the subsequent downstream signaling including ERK1/2 activation and vascular smooth muscle cell proliferation
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
ATP + [ring canal protein]-L-tyrosine
ADP + [ring canal protein]-L-tyrosine phosphate
-
-
-
-
?
ATP + [Runx1]-L-tyrosine
ADP + [Runx1]-L-tyrosine phosphate
the enzyme phosphorylates transcription factor Runx1 and regulates Runx1-mediated megakaryocyte maturation
-
-
?
ATP + [Sam68]-L-tyrosine
ADP + [Sam68]-L-tyrosine phosphate
ATP + [Src-family protein tyrosine kinase]-L-tyrosine
ADP + [Src-family protein tyrosine kinase]-L-tyrosine phosphate
-
i.e. SFK, substrate of protein tyrosine kinases Csk and Chk, phosphorylation at the regulatory tyrosine leading to inhibition of the SFK
-
-
?
ATP + [Stat5B]-L-tyrosine
ADP + [Stat5B]-L-tyrosine phosphate
-
activation by non-receptor tyrosine kinase Pyk2
-
-
?
ATP + [transmembrane adaptor protein LAT]-L-tyrosine
ADP + [transmembrane adaptor protein LAT]-L-tyrosine phosphate
-
substrate of ZAP-70
-
-
?
ATP + [ZAP-70]-L-tyrosine
ADP + [ZAP-70]-L-tyrosine phosphate
-
substrate of Lck, Fyn, and c-Abl, leads to ZAP-70 activation, mechanism
-
-
?
gelsolin + ATP
phospho-tyrosinyl gelsolin + ADP
-
phosphorylation by PYK2 increases the binding of gelsolin to phosphoatidylinositol lipids and actin polymerization at the fibroblastic cell periphery
-
-
?
p130Cas + ATP
phospho-tyrosinyl p130Cas + ADP
-
phosphorylation of the Crk and Nck adaptor protein by Fak
-
-
?
paxillin + ATP
phospho-tyrosinyl paxillin + ADP
-
phosphorylation at Tyr31 and Tyr118 by Fak plays a role in tumor cell motility inhibition
-
-
?
STAT transcription activator protein + ATP
phosphorylated STAT transcription activator protein + ADP
Wiskott-Aldrich syndrome protein + ATP
phospho-tyrosinyl Wiskott-Aldrich syndrome protein + ADP
-
i.e. WASP, phosphorylation by Fak
-
-
?
additional information
?
-
ATP + a protein
ADP + a phosphoprotein
the enzyme controls shoot and floral meristem size
-
-
?
ATP + a protein
ADP + a phosphoprotein
enzyme contributes to signal transduction
-
-
?
ATP + a protein
ADP + a phosphoprotein
enzyme is required in early larval development
-
-
?
ATP + a protein
ADP + a phosphoprotein
-
-
-
-
?
ATP + a protein
ADP + a phosphoprotein
it is likely that LIMK is involved in developmental or oncogenic processes through interactions with these LIM-containing proteins
-
-
?
ATP + a protein
ADP + a phosphoprotein
enzyme plays an important role in spermatogenesis
-
-
?
ATP + a protein
ADP + a phosphoprotein
ILK is a receptor-proximal protein kinase regulating integrin-mediated signal transduction
-
-
?
ATP + a protein
ADP + a phosphoprotein
enzyme is upregulated in HT-144 melanoma cells following TGF-beta1 stimulation
-
-
?
ATP + a protein
ADP + a phosphoprotein
ILK is involved in agonist stimulated, Pi(3)K-dependent, PKB/AKT activation. ILK is thus a receptor-proximal effector for the Pi(3)K-dependent, extracellular matrix and growth factor mediated, activation of PKB/AKT, and inhibition of GSK-3
-
-
?
ATP + a protein
ADP + a phosphoprotein
TESK1 has a specific function in spermatogenesis
-
-
?
ATP + a protein
ADP + a phosphoprotein
the enzyme induces formation of actin stress fibers and focal adhesions
-
-
?
ATP + a protein
ADP + a phosphoprotein
proximal mediators of IL-1 signaling
-
-
?
ATP + a protein
ADP + a phosphoprotein
apoptosis-inducing kinase
-
-
?
ATP + a protein
ADP + a phosphoprotein
NF-kappaB-activating and cell death-inducing kinase
-
-
?
ATP + a protein
ADP + a phosphoprotein
the enzyme is a downstream effector of activated Ras. Interaction with Ras leads to Raf-1 activation and results in transduction of cell growth and differentiation signals
-
-
?
ATP + a protein
ADP + a phosphoprotein
enzyme functions as an intermediary in TNFalpha-induced apoptosis
-
-
?
ATP + a protein
ADP + a phosphoprotein
enzyme plays a critical role in cell growth and development
-
-
?
ATP + a protein
ADP + a phosphoprotein
role for this kinase in spermatogenesis
-
-
?
ATP + a protein
ADP + a phosphoprotein
TESK1 has a specific function in spermatogenesis
-
-
?
ATP + a protein
ADP + a phosphoprotein
the enzyme induces formation of actin stress fibers and focal adhesions
-
-
?
ATP + a protein
ADP + a phosphoprotein
-
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
-
660885, 661230, 661396, 661540, 703984, 703985, 704787, 705448, 705953, 706405, 706765, 706766, 737321, 737757, 738741, 739714 -
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
activation of Syk is responsible for K-Cl cotransport in SS cells by relieving Src-mediated inhibition of the transporter
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
-
-
-
-
?
ATP + Abl
ADP + phospho-L-tyrosinyl-Abl
-
Abl is an important substrate for Src signalling in normal cells
-
-
?
ATP + Abl
ADP + phospho-L-tyrosinyl-Abl
-
Abl is an important substrate for Src signalling in normal cells, Abl is also required for Src-induced transformation of mouse fibroblasts, overview
-
-
?
ATP + Bad protein
ADP + phosphotyrosinyl Bad protein
-
substrate of Akt
-
-
?
ATP + Bad protein
ADP + phosphotyrosinyl Bad protein
-
substrate of Akt
-
-
?
ATP + beta-catenin
ADP + phospho-tyrosinyl-beta-catenin
-
-
-
-
?
ATP + beta-catenin
ADP + phospho-tyrosinyl-beta-catenin
-
-
-
-
?
ATP + beta-catenin
ADP + phospho-tyrosinyl-beta-catenin
-
-
-
-
?
ATP + Cas protein
ADP + phospho-tyrosinyl-Cas protein
-
-
-
-
?
ATP + Cas protein
ADP + phospho-tyrosinyl-Cas protein
-
-
-
-
?
ATP + Cas protein
ADP + phospho-tyrosinyl-Cas protein
-
-
-
-
?
ATP + cortactin
ADP + phospho-tyrosinyl-cortactin
-
-
-
-
?
ATP + cortactin
ADP + phospho-tyrosinyl-cortactin
-
-
-
-
?
ATP + cortactin
ADP + phospho-tyrosinyl-cortactin
-
-
-
-
?
ATP + ezrin
ADP + phospho-tyrosinyl-ezrin
-
-
-
-
?
ATP + ezrin
ADP + phospho-tyrosinyl-ezrin
-
-
-
-
?
ATP + ezrin
ADP + phospho-tyrosinyl-ezrin
-
-
-
-
?
ATP + FAK
ADP + phospho-tyrosinyl-FAK
-
-
-
-
?
ATP + FAK
ADP + phospho-tyrosinyl-FAK
-
-
-
-
?
ATP + FAK
ADP + phospho-tyrosinyl-FAK
-
-
-
-
?
ATP + glycogen synthase kinase 3beta
ADP + phosphotyrosinyl glycogen synthase kinase 3beta
-
substrate of Akt
-
-
?
ATP + glycogen synthase kinase 3beta
ADP + phosphotyrosinyl glycogen synthase kinase 3beta
-
substrate of Akt
-
-
?
ATP + p120 protein
ADP + phospho-tyrosinyl-p120 protein
-
-
-
-
?
ATP + p120 protein
ADP + phospho-tyrosinyl-p120 protein
-
-
-
-
?
ATP + p120 protein
ADP + phospho-tyrosinyl-p120 protein
-
-
-
-
?
ATP + p190 GTPase
ADP + phospho-tyrosinyl-p190 GTPase
-
-
-
-
?
ATP + p190 GTPase
ADP + phospho-tyrosinyl-p190 GTPase
-
-
-
-
?
ATP + p190 GTPase
ADP + phospho-tyrosinyl-p190 GTPase
-
-
-
-
?
ATP + paxillin
ADP + phospho-tyrosinyl-Shc paxillin
-
-
-
-
?
ATP + paxillin
ADP + phospho-tyrosinyl-Shc paxillin
-
-
-
-
?
ATP + paxillin
ADP + phospho-tyrosinyl-Shc paxillin
-
-
-
-
?
ATP + plakoglobin
ADP + phospho-tyrosinyl-plakoglobin
-
-
-
-
?
ATP + plakoglobin
ADP + phospho-tyrosinyl-plakoglobin
-
-
-
-
?
ATP + plakoglobin
ADP + phospho-tyrosinyl-plakoglobin
-
-
-
-
?
ATP + protein
ADP + protein tyrosine phosphate
phosphorylates the regulatory C-terminal tyrosine residue present on cytoplasmic tyrosine kinases of the Src family
-
-
?
ATP + protein
ADP + protein tyrosine phosphate
CSK phosphorylates other members of the src-family of tyrosine kinases at their regulatory carboxy-terminus
-
-
?
ATP + protein tyrosine
ADP + protein tyrosine phosphate
p135tyk2 tyrosine kinase directly binds and tyrosine phosphorylates alpha subunit of the type I IFN receptor, IFN-R
-
-
?
ATP + protein tyrosine
ADP + protein tyrosine phosphate
specifically phosphorylates Tyr527 of p60c-src from neonatal rat brain, specifically phosphorylates a negative regulatory site of p60c-src
-
-
?
ATP + Rho protein
ADP + phospho-tyrosinyl-Rho protein
-
-
-
-
?
ATP + Rho protein
ADP + phospho-tyrosinyl-Rho protein
-
-
-
-
?
ATP + Rho protein
ADP + phospho-tyrosinyl-Rho protein
-
-
-
-
?
ATP + Shc protein
ADP + phospho-tyrosinyl-Shc protein
-
-
-
-
?
ATP + Shc protein
ADP + phospho-tyrosinyl-Shc protein
-
-
-
-
?
ATP + Shc protein
ADP + phospho-tyrosinyl-Shc protein
-
-
-
-
?
ATP + STAT3
ADP + phospho-tyrosinyl-STAT3
-
-
-
-
?
ATP + STAT3
ADP + phospho-tyrosinyl-STAT3
-
-
-
-
?
ATP + STAT3
ADP + phospho-tyrosinyl-STAT3
-
-
-
-
?
ATP + [disabled-1 adaptor protein]-L-tyrosine
ADP + [disabled-1 adaptor protein]-L-tyrosine phosphate
-
activation of disabled-1 adaptor protein Dab1, which is responsible for regulation of neuronal migrations during mammalian brain development, Reelin induces tyrosine-phosphorylated-Dab1 degradation and downregulates Dab1 expression in primary cortical neurons, mutant non-phosphorylated Dab1 are not degraded, pathway regulation, overview
-
-
?
ATP + [disabled-1 adaptor protein]-L-tyrosine
ADP + [disabled-1 adaptor protein]-L-tyrosine phosphate
-
activation of disabled-1 adaptor protein Dab1, which is responsible for regulation of neuronal migrations during mammalian brain development, Reelin induces tyrosine-phosphorylated-Dab1 degradation and downregulates Dab1 expression in primary cortical neurons, mutant non-phosphorylated Dab1 are not degraded, pathway regulation, overview
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
-
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
-
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
-
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
-
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
-
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
-
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
-
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
-
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
-
-
-
?
ATP + [Sam68]-L-tyrosine
ADP + [Sam68]-L-tyrosine phosphate
SRMS regulates the phosphorylation of Sam68 in an EGF-dependent manner in MDA-MB 231 cells
-
-
?
ATP + [Sam68]-L-tyrosine
ADP + [Sam68]-L-tyrosine phosphate
the enzyme (SRMS) regulates the phosphorylation of Sam68 in an EGF-dependent manner in MDA-MB 231 cells
-
-
?
STAT transcription activator protein + ATP
phosphorylated STAT transcription activator protein + ADP
-
activation of STAT by phosphorylation is required for translocation to the nucleus, the enzyme regulates the cytokine expression via STAT, overview
-
-
?
STAT transcription activator protein + ATP
phosphorylated STAT transcription activator protein + ADP
-
activation of STAT by phosphorylation is required for translocation to the nucleus, the enzyme regulates the cytokine expression via STAT, overview
-
-
?
STAT transcription activator protein + ATP
phosphorylated STAT transcription activator protein + ADP
-
activation of STAT by phosphorylation is required for translocation to the nucleus, the enzyme regulates the cytokine expression via STAT, overview
-
-
?
additional information
?
-
oncogene v-fps induces fibrosarcomas in birds
-
-
?
additional information
?
-
-
oncogene v-fps induces fibrosarcomas in birds
-
-
?
additional information
?
-
oncogene v-fps induces fibrosarcomas in birds
-
-
?
additional information
?
-
enzyme can have a protein-protein interaction, through its putative SH3 binding site, with at least two intracellular SH3-containing proteins
-
-
?
additional information
?
-
-
enzyme can have a protein-protein interaction, through its putative SH3 binding site, with at least two intracellular SH3-containing proteins
-
-
?
additional information
?
-
the receptor controls dauer larva development
-
-
?
additional information
?
-
enzyme is involved in TGFbeta signaling
-
-
?
additional information
?
-
cell-surface receptor required for transduction of environmental signals into an appropriate developmental response, controls dauer larva development
-
-
?
additional information
?
-
-
IP3 production in the hypersensitive response of lemon seedlings against Alternaria alternata involves active protein tyrosine kinases but not a G-protein, overview
-
-
?
additional information
?
-
Yes kinase is required during development, overview
-
-
?
additional information
?
-
-
Yes kinase is required during development, overview
-
-
?
additional information
?
-
-
-
-
?
additional information
?
-
-
-
-
-
?
additional information
?
-
required maternally for the establishment of the normal array of embryonic segments
-
-
?
additional information
?
-
plays important roles in cell adhesion, functions downstream of integrins, enzyme is involved in integrin-mediated cell adhesion signaling
-
-
?
additional information
?
-
-
plays important roles in cell adhesion, functions downstream of integrins, enzyme is involved in integrin-mediated cell adhesion signaling
-
-
?
additional information
?
-
mutations in the gene encoding the Drosophila tyrosine kinase Abelson substantially enhanced the severity of the CNS phenotype of armadillo mutations, consistent with these proteins functioning co-operatively at adherens junctions in both the CNS and the epidermis
-
-
?
additional information
?
-
-
Jak2 is involved in transcriptional signaling and ligand-independent gene expression, and increases the activity of erythropoietin receptor cell-surface expression, overview, enzyme deficiency is involved in lymphoid leukemia, overview
-
-
?
additional information
?
-
-
Etk is essential for polymyxin resistance, while Wzc is not
-
-
?
additional information
?
-
-
protein kinases and protein phosphatases regulate enzyme activities in the cell, overview
-
-
?
additional information
?
-
enzyme plays a critical role in a variety of signal transduction pathways
-
-
?
additional information
?
-
-
enzyme plays a critical role in a variety of signal transduction pathways
-
-
?
additional information
?
-
-
Src and Src-family protein-tyrosine kinases are proto-oncogenes important in cell morphology, motility, proliferation, and survival, regulation by reversible phosphorylation, overview
-
-
?
additional information
?
-
-
-
-
?
additional information
?
-
-
-
-
-
?
additional information
?
-
-
-
-
?
additional information
?
-
PTK6 may function as an intracellular signal transducer in specific tissues
-
-
?
additional information
?
-
-
PTK6 may function as an intracellular signal transducer in specific tissues
-
-
?
additional information
?
-
transcriptionally induced in normal T cells by interleukin 2 stimulation, roles in T cell proliferation and differentiation
-
-
?
additional information
?
-
sensitizes mammary epithelial cells to epidermal growth factor
-
-
?
additional information
?
-
-
sensitizes mammary epithelial cells to epidermal growth factor
-
-
?
additional information
?
-
involved in signal transduction by association with a number of membrane receptors
-
-
?
additional information
?
-
enzyme may serve specialized functions in hemopoietic cells, it is possible that damage to HCK may contribute to the pathogenesis of some human leukemias
-
-
?
additional information
?
-
-
enzyme may serve specialized functions in hemopoietic cells, it is possible that damage to HCK may contribute to the pathogenesis of some human leukemias
-
-
?
additional information
?
-
Hck is involved in a number of cell signal transduction pathways, frequently in pathways associated with immune response
-
-
?
additional information
?
-
-
Hck is involved in a number of cell signal transduction pathways, frequently in pathways associated with immune response
-
-
?
additional information
?
-
participates in signal transduction events regulating the growth, differentiation and function of phagocytes
-
-
?
additional information
?
-
it may be involved in key regulatory processes
-
-
?
additional information
?
-
p135tyk2 tyrosine kinase directly binds and tyrosine phosphorylates alpha subunit of the type I IFN receptor, IFN-R. Tyk2 protein functions as part of a receptor complex to initiate intracellular signaling in response to type I interferons
-
-
?
additional information
?
-
-
p135tyk2 tyrosine kinase directly binds and tyrosine phosphorylates alpha subunit of the type I IFN receptor, IFN-R. Tyk2 protein functions as part of a receptor complex to initiate intracellular signaling in response to type I interferons
-
-
?
additional information
?
-
ZAP-70 that associates with T cell antigen receptor zeta chain and undergoes tyrosine phosphorylation following TCR stimulation
-
-
?
additional information
?
-
tandem ZAP-70 SH2 domains bind phosphorylated, but not nonphosphorylated, T cell antigen receptor zeta cyt. The NH2-terminal ZAP-70 SH2 domain also binds to T cell antigen receptor zeta cyt but with 100-fold lower affinity. No binding is observed with the COOH-terminal ZAP-70 SH2 domain. Similar studies demonstrate that the ZAP-70 tandem SH2 domain can bind a T cell antigen receptor zeta 3 TAM peptide in which both tyrosine residues are phosphorylated: Little or no binding is observed with peptides phosphorylated at only one tyrosine residue, or a nonphosphorylated peptide. Binding of the tandem SH2 domains to the other two TCR zeta TAM peptides and to a CD3 epsilon TAM peptide is also observed. All four doubly tyrosine phosphorylated TAM peptides cross-compete with each other for binding to the tandem SH2 domains of ZAP-70. The affinity of these peptides for the tandem SH2 construct demonstrates a hierarchy of TAM zeta 1, TAM zeta 2, TAM epsilon, TAM zeta 3
-
-
?
additional information
?
-
mutations of Jak-3 gene in patients with autosomal severe combined immune deficiency
-
-
?
additional information
?
-
JAK3 deficiency in a patient with severe combined immunodeficiency over 20 years after bone marrow transplantation: persistence of genetically and biochemically defective autologous B cells, associated with reconstitution of cellular and humoral immunity, suggests that integrity of the gammac-JAK3 signalling pathway is not strictly required for immunoglobulin production
-
-
?
additional information
?
-
JAK3 deficiency in humans results in autosomal recessive T-B+ severe combined immunodeficiency disease
-
-
?
additional information
?
-
HYL plays a significant role in the signal transduction of hematopoietic cells
-
-
?
additional information
?
-
-
HYL plays a significant role in the signal transduction of hematopoietic cells
-
-
?
additional information
?
-
enzyme plays a pivotal role in cell signal transduction
-
-
?
additional information
?
-
may play an important role in thymopoiesis, role in controlling cellular growth and differentiation
-
-
?
additional information
?
-
-
may play an important role in thymopoiesis, role in controlling cellular growth and differentiation
-
-
?
additional information
?
-
effector of phosphatidylinositol 3'-kinase and is involved in interleukin 6-induced neuroendocrine differentiation of prostate cancer cells
-
-
?
additional information
?
-
autosomal recessive form of severe combined immunodeficiency disease in which ZAP-70 is absent as a result of mutations in the ZAP-70 gene. This absence is associated with defects in TCR signal transduction. Integral role in T cell activation and differentiation
-
-
?
additional information
?
-
may play a role in the growth and differentiation of hematopoietic cells
-
-
?
additional information
?
-
-
may play a role in the growth and differentiation of hematopoietic cells
-
-
?
additional information
?
-
may have a role in human cancer
-
-
?
additional information
?
-
JAK3 splice isoforms are functional in JAK3 signaling and may enrich the complexity of the intracellular response functional in IL-2 or cytokine signaling
-
-
?
additional information
?
-
mutations of the Janus family kinase JAK3 are responsible for autosomal recessive severe combined immunodeficiency. Abnormalities in tyrosine phosphorylation of JAK3 in response to interleukin-2 (IL-2) and IL-4 is present in all patients. In one patient carrying a single amino acid change, Glu481Gly, in the JH3 domain of JAK3, a partially conserved IL-2 responses is observed resulting in reduced but detectable levels of JAK3 and STAT5 phosphorylation. A single cysteine to arginine substitution, Cys759Arg, results in high basal levels of constitutive JAK3 tyrosine phosphorylation unresponsive to either downregulation by serum starvation or cytokine-mediated upregulation
-
-
?
additional information
?
-
-
mutations of the Janus family kinase JAK3 are responsible for autosomal recessive severe combined immunodeficiency. Abnormalities in tyrosine phosphorylation of JAK3 in response to interleukin-2 (IL-2) and IL-4 is present in all patients. In one patient carrying a single amino acid change, Glu481Gly, in the JH3 domain of JAK3, a partially conserved IL-2 responses is observed resulting in reduced but detectable levels of JAK3 and STAT5 phosphorylation. A single cysteine to arginine substitution, Cys759Arg, results in high basal levels of constitutive JAK3 tyrosine phosphorylation unresponsive to either downregulation by serum starvation or cytokine-mediated upregulation
-
-
?
additional information
?
-
the receptor shares two-hit inactivation mechanism with tumor suppressor genes and mutation of it may occur in the early stage of tumorgenesis
-
-
?
additional information
?
-
mutations in the activin receptor-like kinase 1 gene in hereditary haemorrhagic telangiectasia type 2
-
-
?
additional information
?
-
activin and its receptor play an important role in development
-
-
?
additional information
?
-
the activin receptor-like kinase 1 gene is the second locus for the autosomal dominant vascular disease hereditary hemorrhagic telangiectasia
-
-
?
additional information
?
-
signal transduction by TGF bet involves the formation of a heteromeric complex of two different serine/threonine kinase receptors
-
-
?
additional information
?
-
insensitivity to anti-mullerian hormone is due to a mutation in the human anti-mullerian hormone receptor
-
-
?
additional information
?
-
transforming growth factor-beta regulates cell cycle progression by a unique signaling mechanism that involves its binding to the type II TGF beta receptor and activation of type I
-
-
?
additional information
?
-
-
transforming growth factor-beta regulates cell cycle progression by a unique signaling mechanism that involves its binding to the type II TGF beta receptor and activation of type I
-
-
?
additional information
?
-
enzyme is involved in bone morphogenetic protein signaling
-
-
?
additional information
?
-
-
enzyme is involved in bone morphogenetic protein signaling
-
-
?
additional information
?
-
RIP2 interacts with members of the TNFR-1 signaling complex, including inhibitor of apoptosis protein cIAP1 and with members of the TNFR-associated factor family, specifically TRAF1, TRAF5, and TRAF6, but not with TRAF2, TRAF3, or TRAF4
-
-
?
additional information
?
-
CARDIAK may be involved in NF-kappa B/JNK signaling and in the generation of the proinflammatory cytokine IL-1 beta through activation of caspase-1
-
-
?
additional information
?
-
blocks cell division when overexpressed in Hela cells
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additional information
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activity of WEE1Hu is regulated by phosphorylation and proteolytic degradation, WEE1Hu plays a role in inhibiting mitosis before M phase by phosphorylating cyclin B1-Cdc2
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?
additional information
?
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activity of WEE1Hu is regulated by phosphorylation and proteolytic degradation, WEE1Hu plays a role in inhibiting mitosis before M phase by phosphorylating cyclin B1-Cdc2
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?
additional information
?
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active c-Fes tyrosine kinase binds tubulin and microtubules through separate domains and promotes microtubule assembly, c-Fes colocalization with microtubules in vivo requires the SH2 enzyme domain, implication in the differentiation of vascular, endothelial, myeloid, hematopoietic, and neuronal cells, overview
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?
additional information
?
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ALK-MYH9 performs tyrosine autophosphorylation in vivo, but not in vitro, possible mechanism
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?
additional information
?
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Fes tyrosine kinase promotes survival and terminal granulocyte differentiation of factor-dependent myeloid progenitors (32D) and activates lineage-specific transcription factors, e.g. CCAAT/enhancer-binding protein-alpha and STAT3, down-regulation of macrophage marker F4/80
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?
additional information
?
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JAK2 is an important intracellular mediator of cytokine signalling, JAK2 deficiency may lead to hematologic cancers, and a number of immune diseases
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?
additional information
?
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protein tyrosine kinases are involved in downstream signaling pathways, e.g. BCR/ABL kinase in the phosphatidylinositol 3'-kinase pathway, required for regulation of cell differentiation and cell cycle regulation, BCR/ABL and several other constitutive protein tyrosine kinases are activated in myeloid malignancies, overview, protein deregulation probable due to fusion gene formation because of chromosomal translocations or as distinct gain-of-function point mutations, autophosphorylation of BCR/ABL kinase at Tyr177 is essential for myeloid leukomogenesis in vivo, expression of BCR/ABL kinase leads to functional downregulation of the basal transcription factor TFIIH involved in nucleotide excision DNA repair pathway, and to activation of RAD51 also involved in DNA repair, overview
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?
additional information
?
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protein tyrosine kinases play a critical role in the modulation of a wide range of cellular events such as cell division, cell differentiation, and cell metabolism, over-stimulation of PTKs impairs normal cell growth, resulting in oncogenic transformation, regulation of enzyme activity occurs in dynamic oscillatory behaviour, patterns and mechanism, overview
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?
additional information
?
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PTKs are involved in cell signalling
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?
additional information
?
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spleen tyrosine kinase Syk modulates epidermal growth factor receptor EGFR signalling in mammary epithelial cells acting as a negative controle element, regulation of EGFR by activation of the autophosphorylation activity of EGFR, but not of HER2 and HER3, overview
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?
additional information
?
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Src and Src-family protein-tyrosine kinases are proto-oncogenes important in cell morphology, motility, proliferation, and survival, regulation by reversible phosphorylation, overview
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?
additional information
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Src-dependent outside-in signalling is a key step in the process of autoregulation of beta2 integrins in polymorphonuclear cells and required for adhesion of interleukin-8, Src PTKs are required for macrophage antigen-1-mediated adhesion, which is inhibited by cytochalasin D and involved F-actin and protein P-110, overview
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?
additional information
?
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Src-family protein tyrosine kinases are proto-oncogenic enzymes controlling mammalian cell growth and proliferation, the enzymes are regulated by activation through autophosphorylation of their kinase domain and by inhibition through phosphorylation of their regulatory tyrosine residue near the C-terminus, mechanism, overview, abberrant SFK activation contributes to cancer development
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?
additional information
?
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Syk kinase is involved in cell motility and activation of phosphatidylinositol 3'-kinase, Syk kinase inhibits the tyrosine phosphorylation of IkappaBalpha and thus inhibits activation of NFkappaB via interaction of IkappaBalpha and phosphatidylinositol 3'-kinase, pathway regulation, overview
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?
additional information
?
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Tec family tyrosine kinases play a central role in hematopoietic cellular signaling
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?
additional information
?
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the enzyme is regulated in balance with protein tyrosine phosphatase, complex regulation mechanism, overview, the enzyme has decreasing effect, opposing to receptor protein tyrosine kinase EGFR, on volume-sensitive chloride current in atrial myocytes, overview
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?
additional information
?
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the Fes tyrosine kinase is regulated via its SH2 domain
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?
additional information
?
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the Janus kinase is involved in the JAK-STAT signaling cascade causing inflammatory activity in the brain
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?
additional information
?
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the Src tyrosine kinase regulates and stimulates silica particle formation in lung epithelium which induces interleukin-8 release activating the signaling cascade via phosphorylation of MAPK and ERK, overview
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?
additional information
?
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the Syk family tyrosine kinase ZAP-70 is required to couple the activated T-cell antigen receptor TCR to downstream signaling pathways, binding of TCR via its SH2 domains, regulation mechanism, overview
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?
additional information
?
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a multisite model for Fyn binding and regulation, overview, subtype-selective modulation by tyrosine phosphorylation/dephosphorylation provides a mechanism for differential regulation of sodium channels by neurotrophins and tyrosine phosphorylation in unmyelinated axons and dendrites, where NaV1.2 channels are expressed in brain neurons, overview
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?
additional information
?
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Brutons tyrosine kinase is involved in B lymphocyte chemotaxis and homing, overview
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?
additional information
?
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c-Abl activates p21 transcription via interaction with and regulation of the DNA-binding of p53, c-Abl also recruits p53 to the p21 promoter, overview
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?
additional information
?
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c-Abl is regulated by conformational changes through intramolecular interactions and phosphorylation, overview
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?
additional information
?
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c-Src is a physiologically relevant substrate for Methionine aminopeptidases, whose dysfunction is likely to account for the cell-cycle effects of MetAP inhibitors including bengamide A, overview
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?
additional information
?
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dynamics of BCR-ABL kinase domain mutations in chronic myeloid leukemia after sequential treatment with multiple tyrosine kinase inhibitors, overview
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?
additional information
?
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dynamics of BCR-ABL kinase domain mutations in chronic myeloid leukemia after sequential treatment with multiple tyrosine kinase inhibitors, overview
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?
additional information
?
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enzyme deficiency leads to X-linked agammaglobulinemia, XLA, a humoral primary immunodeficiency in which affected patients have very low levels of peripheral B cells and a profound deficiency of all immunoglobulin isotypes, overview
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?
additional information
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enzyme deficiency leads to X-linked agammaglobulinemia, XLA, a humoral primary immunodeficiency in which affected patients have very low levels of peripheral B cells and a profound deficiency of all immunoglobulin isotypes, overview
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?
additional information
?
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FAK plays a role in the anoikis phenomenon or anchorage-dependent cell survival, and in angiogenesis and formation of new blood vessels, overview, downstream targets of the FAK and PYK2 are MAP kinases implicated in proliferative processes, PYK2 is an essential linker between G-protein coupled receptor and the MAPK cascade, overview
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?
additional information
?
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Fes is involved in the regulation of cell-cell and cell-matrix interactions mediated by adherens junctions and focal adhesions, the activated form of the kinase can induce cellular transformation, overview
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?
additional information
?
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Fyn tyrosine kinase is involved in actin stress fiber formation in fibroblasts
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?
additional information
?
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Jak2 is involved in transcriptional signaling and ligand-independent gene expression, and increases the activity of erythropoietin receptor cell-surface expression, overview, enzyme deficiency is involved in lymphoid leukemia, overview
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-
?
additional information
?
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p38 MAP kinase inhibitor SB203580 and protein tyrosine kinase inhibitor tyrphostin 25 combined can be used for inhibition of matrix metalloproteinase-9 expression, overview
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?
additional information
?
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protein-tyrosine kinase Syk plays a central role in Fcgamma receptor-mediated phagocytosis in the adaptive immune system, and is required for pathogen engulfment in complement-mediated phagocytosis
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?
additional information
?
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Src and Abl regulation, overview, cytoplasmic tyrosine kinase Src is involved in signal transduction induced by growth factors and integrins, Src also shows oncogenic activity when it is deregulated, Abl mediates Src-induced extracellular regulated kinase 5, ERK5, activation to drive cell transformation, Abl/Rac and Abl/ERK5 pathways also operate in human MCF7 and BT549 breast cancer cells, where neoplastic transformation depends on Src-like activities, overview
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?
additional information
?
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Src PTK plays a role in NF-kappaB activation in epithelial cells, Src PTKs are important in regulation of vascular permeability and acute inflammatory responses, and are essential for the recruitment and activation of monocytes, macrophages, neutrophils, and other immune cells, Src PTKs can also regulate the functional activity of these receptors and is involved in cell signaling, biological functions, cellular and molecular mechanisms, overview
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?
additional information
?
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Syk protein tyrosine kinase is involved in lipopolysaccharide-induced responses and intracellular signaling leading to release of pro-inflammatory mediators in macrophages, overview
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?
additional information
?
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the BCR-ABL tyrosine kinase is inhibited in Philadelphia chromosome-positive chronic myeloid leukemia, CML, overview
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?
additional information
?
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the enzyme tyrosine phosphorylates a wide range of proteins, especially nuclear matrix proteins
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?
additional information
?
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the Src family of protein kinases mediates mitogenic signal transduction, and constitutive activation of the enzymes is associated with tumorigenesis
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?
additional information
?
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the Src protein tyrosine kinase p56Lck plays a critical role in the O2 sensitivity of Kv1.3 channels and in signalling during hypoxia in T lymphocytes, overview
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?
additional information
?
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the Src-family tyrosine kinase fyn phosphorylates phosphatidylinositol 3-kinase enhancer-activating Akt, preventing its apoptotic cleavage and promoting cell survival, overview
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?
additional information
?
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Toll-like receptors TLR-8 and TLR-9 require activation/phosphorylation by Btk for acting incell signaling, overview, enzyme deficiency is involved in development of male immune disorder X-linked agammaglobulineamia, XLA
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?
additional information
?
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tyrosine kinase Src is a key enzyme in mammalian signal transduction and an important target for anticancer drug discovery
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-
?
additional information
?
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tyrosine kinases play a fundamental role in cell proliferation, survival, adhesion, and motility and have also been shown to mediate malignant cell transformation, Brk may play a key role in lymphomagenesis
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?
additional information
?
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role for JAK3 in hematopoiesis and T- and B-cell development
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?
additional information
?
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involvement of the Jak-3 Janus kinase in signalling by interleukins 2 and 4 in lymphoid and myeloid cells
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?
additional information
?
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JAK3 kinase is associated with terminal differentiation of hematopoietic cells
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?
additional information
?
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the enzyme transduces signals initiated by integrin engagement and G protein-coupled receptors. Several splice isoforms of FAK are preferentially expressed in rat brain, some of which have an increased autophosphorylation activity
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?
additional information
?
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activation of FadK may be an important early step in intracellular signal transduction pathways triggered in response to cell interactions with the extracellular matrix
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?
additional information
?
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activation of FadK may be an important early step in intracellular signal transduction pathways triggered in response to cell interactions with the extracellular matrix
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?
additional information
?
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lskT-encoded protein-tyrosine kinase may aid in transducing proliferative or differentiative signals unique to lymphocytes
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?
additional information
?
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lskT-encoded protein-tyrosine kinase may aid in transducing proliferative or differentiative signals unique to lymphocytes
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?
additional information
?
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enzyme is implicated in neoplastic transformation
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?
additional information
?
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enzyme is implicated in neoplastic transformation
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?
additional information
?
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enzyme is involved in pathway for signaling through glycosyl-phosphatidylinositol (GPI)-anchored membrane proteins
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?
additional information
?
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elevated levels of p56tck can contribute to the malignant properties of LSTRA cells
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?
additional information
?
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elevated levels of p56tck can contribute to the malignant properties of LSTRA cells
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?
additional information
?
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p56lck can positively regulate T-cell functions and it mediates at least some of the effects of CD4 and CD8 on T-cell activation
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?
additional information
?
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p56lck can positively regulate T-cell functions and it mediates at least some of the effects of CD4 and CD8 on T-cell activation
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?
additional information
?
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p56lck participates in lymphocyte-specific signal transduction pathways. Disturbances in lck expression may contribute to the pathogenesis of some human neoplastic diseases
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?
additional information
?
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p56lck participates in lymphocyte-specific signal transduction pathways. Disturbances in lck expression may contribute to the pathogenesis of some human neoplastic diseases
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?
additional information
?
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may be specifically involved in the cell growth of hepatocytes or in the step of hepatocarcinogenesis
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?
additional information
?
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may be specifically involved in the cell growth of hepatocytes or in the step of hepatocarcinogenesis
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?
additional information
?
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may interact with the intracellular domain of cell surface receptors
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?
additional information
?
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participates in the signalling pathways of a broad range of cytokines
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?
additional information
?
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participates in the signalling pathways of a broad range of cytokines
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?
additional information
?
-
enzyme is crucial for B cell development. Loss of kinase activity results in the human immunodeficiency, X-linked agammaglobulinemia, characterized by a failure to produce B cells
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?
additional information
?
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enzyme is crucial for B cell development. Loss of kinase activity results in the human immunodeficiency, X-linked agammaglobulinemia, characterized by a failure to produce B cells
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-
?
additional information
?
-
directly implicated in the pathogenesis of X-linked agammaglobulinaemia
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?
additional information
?
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-
directly implicated in the pathogenesis of X-linked agammaglobulinaemia
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?
additional information
?
-
deficient expression of a B cell cytoplasmic tyrosine kinase in human X-linked agammaglobulinemia
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?
additional information
?
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perinatal lethality and blocked B-cell development in mice lacking the tyrosine kinase Syk. Syk-deficient radiation chimaeras fail to accumulate mature B cells, Syk-deficient mice show impaired development of thymocytes using the V gamma 3 variable region gene, Syk is not required for signalling through the IL-2 and G-CSF receptors
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-
?
additional information
?
-
Rlk has potential functions in intrathymic T cell development and mature T cell signaling
-
-
?
additional information
?
-
Ntk may play an inhibitory role in the control of T-cell proliferation
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-
?
additional information
?
-
role for JAK1 kinase in the differentiation or function of a subset of CNS neurons
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-
?
additional information
?
-
-
role for JAK1 kinase in the differentiation or function of a subset of CNS neurons
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-
?
additional information
?
-
activating motif occurs in four discrete steps: binding of p59fyn, phosphorylation of the motif, binding of ZAP-70, and activation of ZAP-70 kinase activity
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-
?
additional information
?
-
Ctk is involved in the regulation of neural function and differentiation of male germ cells through interactions with members of the Src family kinases
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-
?
additional information
?
-
could be responsible for the tyrosine phosphorylation observed in a murine thymic medullary epithelial cell line E-5 following complex formation with thymocytes
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-
?
additional information
?
-
type II receptor isoforma exist which play preferential binding to TGF-beta2 and have their own defined role in debvelopment
-
-
?
additional information
?
-
mRIP3 uses a novel mechanism to induce death
-
-
?
additional information
?
-
-
mRIP3 uses a novel mechanism to induce death
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?
additional information
?
-
in a cell cycle the wee1 kinase is phosphorylated at M-phase, phosphorylation occurs in the N-terminal domain resulting in inactivation of the kinase activity. The N-terminal domain, or the entire molecule is extensively phosphorylated by cdc2-cyclin B kinase
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?
additional information
?
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CX3CL1, i.e. fractalkine, only member of the delta subclass of chemokines, triggers PTK Syk activity in monocytes/macrophages localized in F-actin-enriched cell protrusions, which are formed due to CX3CL1 treatment and subsequent increase in F-actin, Syk deficiency results in strong impairment of RAW cell migration to CX3CL1, overview
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?
additional information
?
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-
Fps/Fes and Fer protein-tyrosine kinases play redundant roles in regulating hematopoiesis
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?
additional information
?
-
-
Fps/Fes tyrosine kinase is involved in regulation of erythropoiesis and of myeloid differentiation and survival
-
-
?
additional information
?
-
-
protein tyrosine kinases are involved in downstream signaling pathways, e.g. BCR/ABL kinase in the phosphatidylinositol 3'-kinase pathway, required for regulation of cell differentiation and cell cycle regulation, expression of BCR/ABL kinase leads to functional downregulation of the basal transcription factor TFIIH involved in nucleotide excision DNA repair pathway, and to activation of RAD51 also involved in DNA repair, overview
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-
?
additional information
?
-
-
Src family kinases Hck, Fyn and Src are constitutively expressed and are required for murine embryonic stem cell growth and differentiation, regulation of SFKs in response to leukemia inhibitory factor LIF and other growth factors, overview
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?
additional information
?
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the enzyme plays an important role in the self-renewal and as comitogen in the movement of stem cells out of the haematopoietic stem cell pool into the progeny pool, regulation of bone marrow cell migration
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-
?
additional information
?
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Brutons tyrosine kinase is involved in B lymphocyte chemotaxis and homing, overview
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-
?
additional information
?
-
-
Csk is essential for mouse embryonic development, Csk plays a role in G protein-coupled receptor- and receptor tyrosine kinase-induced fibroblast cell migration, overview, modeling of Csk regulation of focal adhesion turnover
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-
?
additional information
?
-
-
enzyme-deficient endothelial cells shows reduced migration, as well as decreased cell proliferation and survival in vivo
-
-
?
additional information
?
-
-
Jak2 is involved in transcriptional signaling and ligand-independent gene expression, and increases the activity of erythropoietin receptor cell-surface expression, overview, enzyme deficiency is involved in lymphoid leukemia, overview
-
-
?
additional information
?
-
-
PYK2 is involved in vascular endothelial growth factor-induced activities, such as cell migration, blood vessel formation, Pyk2 forms complexes with Src tyrosine kinase for activation of the Akt tyrosine kinase pathway, PYK2 is required in receptor- and ischemia-activated signaling events leading to endothelial NO synthase phosphorylation and modulation of endothelial NO synthase-mediated vasoactive function and angiogenic response, PYK2 is involved in Ca2+ mobilization in muscle cells, overview
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-
?
additional information
?
-
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spleen tyrosine kinase Syk is necessary for E-selectin-induced alpha(L)beta(2) integrin-mediated rolling on intercellular adhesion molecule-1, neutrophil activation pathways, overview
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-
?
additional information
?
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Src and Abl regulation, overview, cytoplasmic tyrosine kinase Src is involved in signal transduction induced by growth factors and integrins, Src also shows oncogenic activity when it is deregulated, Abl mediates Src-induced extracellular regulated kinase 5, ERK5, activation to drive cell transformation
-
-
?
additional information
?
-
-
Src PTK plays a role in NF-kappaB activation in epithelial cells, Src PTKs are important in regulation of vascular permeability and acute inflammatory responses, and are essential for the recruitment and activation of monocytes, macrophages, neutrophils, and other immune cells, Src PTKs can also regulate the functional activity of these receptors and is involved in cell signaling, biological functions, cellular and molecular mechanisms, overview
-
-
?
additional information
?
-
-
the Brutons tyrosine kinase is a critical signaling mediator downstream of the B cell Ag receptor, plays a role in regulating TLR-induced cytokine production, and is required for TLR-induced IL-10 production in multiple macrophage populations and in TLR signaling, overview, X-linked agammaglobulinemia is caused by mutations in Btk resulting in multiple defects in B cell development and function, and recurrent bacterial infections, Btk-dependent induction of NFkappaB and AP-1 DNA binding activity
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-
?
additional information
?
-
the enzyme is involved in cytokine signaling
-
-
?
additional information
?
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-
the enzyme is involved in cytokine signaling
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?
additional information
?
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tyrosine kinase Fyn determines the specific localization of TrkB brain-derived neurotrophic factor, BDNF, receptor to intracellular lipid rafts in cortical and hippocampal membranes, this process is critically dependent on the tyrosine kinase Fyn, overview, role for lipid rafts in neurotrophin signaling
-
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?
additional information
?
-
-
the Brutons tyrosine kinase is a critical signaling mediator downstream of the B cell Ag receptor, plays a role in regulating TLR-induced cytokine production, and is required for TLR-induced IL-10 production in multiple macrophage populations and in TLR signaling, overview, X-linked agammaglobulinemia is caused by mutations in Btk resulting in multiple defects in B cell development and function, and recurrent bacterial infections, Btk-dependent induction of NFkappaB and AP-1 DNA binding activity
-
-
?
additional information
?
-
-
enzyme is involved in cell growth, differentiation, and apoptosis
-
-
?
additional information
?
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-
antagonistic regulation of swelling-activated Cl- current in rabbit ventricle by Src and EGFR protein tyrosine kinases, overview
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?
additional information
?
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Src activates an outwardly rectifying chloride current in myocytes being involved in osmotic swelling, enzyme inhibition also inhibits stretch-activated Cl- current, mechanism, overview
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-
?
additional information
?
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Lyn is an important B cell signaling kinase of the Src tyrosine kinase family with a broad range of functions from cytoskeletal changes to induction of apoptosis, Lyn and and its interaction with rafts and TLR2 are involved in the initial stages of Pseudomonas aeruginosa interaction with host cells and invasion of an alveolar epithelial cell line, primary lung cells, and rat lungs by Pseudomonas aeruginosa, overview
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-
?
additional information
?
-
specifically phosphorylates Tyr527 of p60c-src from neonatal rat brain. Specifically phosphorylates a negative regulatory site of p60c-src
-
-
?
additional information
?
-
CSK is involved in regulation of src family kinases
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-
?
additional information
?
-
Batk may function as a brain-specific regulator of kinases involved in the development and maintenance of the nervous system
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-
?
additional information
?
-
appear to play a role in B-cell-IgM and FcERI receptor signaling
-
-
?
additional information
?
-
TGF-beta RII expression is down-regulated in cells treated with exogenous TGF-beta1
-
-
?
additional information
?
-
mullerian inhibiting substance causes regression of the fetal Mullerian duct on binding a heteromeric complex of types I and II cell-surface receptors in the fetal urogenital ridge. The anti-mullerian hormone type II receptor provides specificity for mullerian inhibiting substance
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-
?
additional information
?
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protein tyrosine kinase-dependent modulation of voltage-dependent potassium channels by genistein in cardiac ventricular myocytes
-
-
?
additional information
?
-
-
the Src tyrosine kinase regulates and stimulates silica particle formation in epithelium which induces chemokine KIP-2 release activating the signaling cascade via phosphorylation of MAPK and ERK, overview
-
-
?
additional information
?
-
-
Src PTK plays a role in NF-kappaB activation in epithelial cells, Src PTKs are important in regulation of vascular permeability and acute inflammatory responses, and are essential for the recruitment and activation of monocytes, macrophages, neutrophils, and other immune cells, Src PTKs can also regulate the functional activity of these receptors and is involved in cell signaling, biological functions, cellular and molecular mechanisms, overview
-
-
?
additional information
?
-
-
Syk protein tyrosine kinase is involved in lipopolysaccharide-induced responses and intracellular signaling leading to release of pro-inflammatory mediators in macrophages, overview
-
-
?
additional information
?
-
-
tyrosine kinase Fyn determines the specific localization of TrkB brain-derived neurotrophic factor, BDNF, receptor in to intracellular lipid rafts in cortical and hippocampal membranes, this process is critically dependent on the tyrosine kinase Fyn, overview, role for lipid rafts in neurotrophin signaling
-
-
?
additional information
?
-
associated with breast cancer and osteoporosis
-
-
?
additional information
?
-
-
Src and Src-family protein-tyrosine kinases are proto-oncogenes important in cell morphology, motility, proliferation, and survival, regulation by reversible phosphorylation, overview
-
-
?
additional information
?
-
-
the enzyme is involved in regulation of sperm capacitation, signal transduction mechanism, capacitation mechanism, overview
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-
?
additional information
?
-
is likely to participate in a variety of integrin-extracellular-matrix-dependent signaling events during morphogenesis
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-
?
additional information
?
-
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is likely to participate in a variety of integrin-extracellular-matrix-dependent signaling events during morphogenesis
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-
?
additional information
?
-
participate in signalling pathways activated in response to cell interaction, role for FAK in gastrulation
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?
additional information
?
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participate in signalling pathways activated in response to cell interaction, role for FAK in gastrulation
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?
additional information
?
-
yes gene product is likely to play an important role in oogenesis or early development
-
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?
additional information
?
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functions during reinitiation of meiotic division
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-
?
additional information
?
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the kinase induces progression through the cell cycle for both meiotic and mitotic cells
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?
additional information
?
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involved in signal transduction
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-
?
additional information
?
-
importance of the function of activin receptor in the regulatory mechanism for body axis formation
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?
additional information
?
-
down-regulation of Wee1-like kinase activity by phosphorylation at mitosis is a multistep process that occurs after other biochemical reactions have signaled the successful completion of S phase
-
-
?
additional information
?
-
possible function during secondary steps of tumor progression
-
-
?
additional information
?
-
possible function during secondary steps of tumor progression
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-
?
additional information
?
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-
possible function during secondary steps of tumor progression
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?
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(2-[2-[(3,5-dimethylphenyl)amino]pyrimidin-4-yl]-1,3-thiazol-4-yl)methanol
-
-
(2-[2-[(3,5-dimethylphenyl)amino]pyrimidin-4-yl]-1,3-thiazol-5-yl)methanol
-
-
(2E)-3-(6-bromopyridin-2-yl)-2-cyano-N-[(1S)-1-phenylethyl]prop-2-enamide
-
WP1066
(2E)-N-benzyl-2-cyano-3-(3,4-dihydroxyphenyl)prop-2-enamide
-
LS104
(2E,4E)-N-benzyl-2-cyano-5-(3,4-dihydroxyphenyl)penta-2,4-dienamide
-
AG490, potent JAK2 inhibitor
(4E,6Z,8S,9S,10E,12S,13R,14S,16S,17R)-8,13,14,17-tetramethoxy-4,10,12,16-tetramethyl-3,20,22-trioxo-2-azabicyclo[16.3.1]docosa-1(21),4,6,10,18-pentaen-9-yl carbamate
-
indirect pharmacological inhibitor
1-(4-((5-methyl-2-((4-morpholinophenyl)amino)pyrimidin-4-yl) amino)piperidin-1-yl)ethan-1-one
100 nM, 70.5% inhibition. 28°C, pH not specified in the publication
1-(4-(5-methyl-2-((4-morpholinophenyl)amino)pyrimidin-4-yl) piperazin-1-yl)ethan-1-one
100 nM, 66.2% inhibition. 28°C, pH not specified in the publication
1-(4-(5-methyl-2-((4-morpholinophenyl)amino)pyrimidin-4-yl) piperazin-1-yl)pentane-1,4-dione
100 nM, 56.4% inhibition. 28°C, pH not specified in the publication
1-(4-(5-methyl-2-((4-morpholinophenyl)amino)pyrimidin-4-yl) piperazin-1-yl)propan-1-one
100 nM, 73.4% inhibition. 28°C, pH not specified in the publication
1-(4-acetylphenyl)-3-(1-(5-methyl-2-((4-morpholinophenyl) amino)pyrimidin-4-yl)azetidin-3-yl)urea
100 nM, 21.9% inhibition. 28°C, pH not specified in the publication
1-(4-acetylphenyl)-3-(1-(5-methyl-2-((4-morpholinophenyl) amino)pyrimidin-4-yl)pyrrolidin-3-yl)urea
100 nM, 57.4% inhibition. 28°C, pH not specified in the publication
1-(4-[5-(4-ethoxybenzoyl)-6-[(propan-2-yl)amino]pyrimidin-4-yl]piperazin-1-yl)prop-2-en-1-one
inhibitory rate at 0.01 mM is 24.04%
1-(4-[5-(4-phenoxybenzoyl)-6-[(propan-2-yl)amino]pyrimidin-4-yl]piperazin-1-yl)prop-2-en-1-one
inhibitory rate at 0.01 mM is 48.54%
1-(4-[6-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]-2-methylpyrimidin-4-yl]piperazin-1-yl)-3-(1-nonadecyl-1H-1,2,3-triazol-4-yl)propan-1-one
-
1-(4-[[5-(4-ethoxybenzoyl)-6-(ethylamino)pyrimidin-4-yl]amino]piperidin-1-yl)prop-2-en-1-one
inhibitory rate at 0.01 mM is 6.81%
1-(4-[[5-(4-ethoxybenzoyl)-6-(methylamino)pyrimidin-4-yl]amino]piperidin-1-yl)prop-2-en-1-one
inhibitory rate at 0.01 mM is %
1-(4-[[6-(dimethylamino)-5-(4-ethoxybenzoyl)pyrimidin-4-yl]amino]piperidin-1-yl)prop-2-en-1-one
inhibitory rate at 0.01 mM is 9.8%
1-(4-[[6-(ethylamino)-5-(4-phenoxybenzoyl)pyrimidin-4-yl]amino]piperidin-1-yl)prop-2-en-1-one
inhibitory rate at 0.01 mM is %
1-(4-[[6-(methylamino)-5-(4-phenoxybenzoyl)pyrimidin-4-yl]amino]piperidin-1-yl)prop-2-en-1-one
inhibitory rate at 0.01 mM is 10.61%
1-(4-[[6-amino-5-(4-phenoxybenzoyl)pyrimidin-4-yl]amino]piperidin-1-yl)prop-2-en-1-one
inhibitory rate at 0.01 mM is 78.13%
1-azaanthraquinones
-
-
-
1-methyl-emodin
-
inhibition of p56lck and c-Src
1-[(3R)-3-([5-(4-phenoxybenzoyl)-6-[(propan-2-yl)amino]pyrimidin-4-yl]amino)piperidin-1-yl]prop-2-en-1-one
inhibitory rate at 0.01 mM is 14.56%
1-[(3R)-3-[[5-(4-ethoxybenzoyl)-6-(methylamino)pyrimidin-4-yl]amino]piperidin-1-yl]prop-2-en-1-one
inhibitory rate at 0.01 mM is 10.27%
1-[(3R)-3-[[5-(4-phenoxybenzoyl)-6-(piperidin-1-yl)pyrimidin-4-yl]amino]piperidin-1-yl]prop-2-en-1-one
inhibitory rate at 0.01 mM is 15.67%
1-[(3R)-3-[[6-(dimethylamino)-5-(4-phenoxybenzoyl)pyrimidin-4-yl]amino]piperidin-1-yl]prop-2-en-1-one
inhibitory rate at 0.01 mM is 11.42%
1-[(3R)-3-[[6-(ethylamino)-5-(4-phenoxybenzoyl)pyrimidin-4-yl]amino]piperidin-1-yl]prop-2-en-1-one
inhibitory rate at 0.01 mM is 18.24%
1-[(3R)-3-[[6-(methylamino)-5-(4-phenoxybenzoyl)pyrimidin-4-yl]amino]piperidin-1-yl]prop-2-en-1-one
inhibitory rate at 0.01 mM is 6.66%
1-[(3R)-3-[[6-amino-5-(4-ethoxybenzoyl)pyrimidin-4-yl]amino]piperidin-1-yl]prop-2-en-1-one
inhibitory rate at 0.01 mM is 52.88%
1-[(3R)-3-[[6-amino-5-(4-phenoxybenzoyl)pyrimidin-4-yl]amino]piperidin-1-yl]prop-2-en-1-one
inhibitory rate at 0.01 mM is 100%
1-[4-([5-(4-ethoxybenzoyl)-6-[(propan-2-yl)amino]pyrimidin-4-yl]amino)piperidin-1-yl]prop-2-en-1-one
inhibitory rate at 0.01 mM is 8.69%
1-[4-([5-(4-phenoxybenzoyl)-6-[(propan-2-yl)amino]pyrimidin-4-yl]amino)piperidin-1-yl]prop-2-en-1-one
inhibitory rate at 0.01 mM is 1.2%
1-[4-[5-(4-ethoxybenzoyl)-6-(ethylamino)pyrimidin-4-yl]piperazin-1-yl]prop-2-en-1-one
inhibitory rate at 0.01 mM is 6.43%
1-[4-[5-(4-ethoxybenzoyl)-6-(methylamino)pyrimidin-4-yl]piperazin-1-yl]prop-2-en-1-one
inhibitory rate at 0.01 mM is 11-87%
1-[4-[6-(ethylamino)-5-(4-phenoxybenzoyl)pyrimidin-4-yl]piperazin-1-yl]prop-2-en-1-one
inhibitory rate at 0.01 mM is 17.53%
1-[4-[6-(methylamino)-5-(4-phenoxybenzoyl)pyrimidin-4-yl]piperazin-1-yl]prop-2-en-1-one
inhibitory rate at 0.01 mM is 8.14%
1-[4-[6-amino-5-(4-ethoxybenzoyl)pyrimidin-4-yl]piperazin-1-yl]prop-2-en-1-one
inhibitory rate at 0.01 mM is 87.67 %
1-[4-[6-amino-5-(4-phenoxybenzoyl)pyrimidin-4-yl]piperazin-1-yl]prop-2-en-1-one
inhibitory rate at 0.01 mM is 93.21%
2,5-dihydroxy methyl cinnamate
-
i.e. DHMC, PTK inhibitor, prevents the IP3 production in lemon seedlings in response to fungal attack and blocks the development of hypersensitive response
2,5-dihydroxy-3-(3,4-dihydroxyphenyl)-6-phenyl-1,4-benzoquinone
-
secondary metabolite isolated from fungus Stilbella sp. strain 1586
2,5-dihydroxy-3-phenyl-6-(3,4,5-trihydroxyphenyl)-1,4-benzoquinone
-
secondary metabolite isolated from fungus Stilbella sp. strain 1586
2,7,8-trihydroxy-3-phenyl-1,4-dibenzofurandione
-
secondary metabolite isolated from fungus Stilbella sp. strain 1586
2-(1,1-dimethylethyl)-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinolin-7-one
-
i.e. JAK inhibitor-I
2-(2-[2-[(3,5-dimethylphenyl)amino]pyrimidin-4-yl]-4-methyl-1,3-thiazol-5-yl)ethanol
-
-
2-(4-acetylphenyl)-1-(4-(2-((4-morpholinophenyl)amino)thieno[3,2-d]pyrimidin-4-yl)piperazin-1-yl)ethan-1-one
100 nM, 44% inhibition. 28°C, pH not specified in the publication
2-([4-[(5-chloro-1,3-benzodioxol-4-yl)amino]pyrimidin-2-yl]amino)benzenesulfonamide
-
-
2-([4-[(5-chloro-1,3-benzodioxol-4-yl)amino]pyrimidin-2-yl]amino)benzonitrile
-
-
2-chloro-N-[5-[(3-chlorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
2-chloro-N-[5-[(3-fluorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
2-chloro-N-[5-[(4-fluorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
2-chloro-N-[5-[(4-methoxybenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
2-chloro-N-[5-[(4-nitrobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
2-chloro-omega-hydroxy-emodin
-
inhibition of p56lck and c-Src
2-cyclopentyl-9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-9H-purin-6-amine
-
2-tert-butyl-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinoline-7-one
-
potent pan-JAK inhibitor
2-[2-[(3,5-dimethylphenyl)amino]pyrimidin-4-yl]-N-[(1R)-2-hydroxy-1-methylethyl]-4-methyl-1,3-thiazole-5-carboxamide
-
-
2-[2-[(3,5-dimethylphenyl)amino]pyrimidin-4-yl]-N-[(1S)-2-hydroxy-1-methylethyl]-4-methyl-1,3-thiazole-5-carboxamide
-
-
2-[4-methyl-2-(2-[[3-methyl-5-(trifluoromethyl)phenyl]amino]pyrimidin-4-yl)-1,3-thiazol-5-yl]ethanol
-
-
3-(9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-6-[[4-(dimethylphosphoryl)phenyl]amino]-9H-purin-2-yl)propanenitrile
-
3-([4-[(5-chloro-1,3-benzodioxol-4-yl)amino]pyrimidin-2-yl]amino)benzenesulfonamide
-
-
3-([4-[(5-chloro-1,3-benzodioxol-4-yl)amino]pyrimidin-2-yl]amino)benzonitrile
-
-
3-([4-[4-(hydroxymethyl)-1,3-thiazol-2-yl]pyrimidin-2-yl]amino)-5-(trifluoromethyl)phenol
-
-
3-amino-5-((2R)-3-methylbutan-2-yl)-7-[5-(morpholin-4-yl)-pyridin-2-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
-
3-amino-5-((2S)-3-methylbutan-2-yl)-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
-
3-amino-5-((2S)-3-methylbutan-2-yl)-7-[1-methyl-5-(morpholin-4-yl)-1H-pyrazol-3-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
-
3-amino-5-((2S)-3-methylbutan-2-yl)-7-[1-methyl-5-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-3-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]-pyridin-4-one
-
3-amino-5-((2S)-3-methylbutan-2-yl)-7-[5-(morpholin-4-yl)-pyridin-2-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
-
3-amino-5-(2-methylpentan-3-yl)-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
-
3-amino-5-(3-methylbutan-2-yl)-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
-
3-amino-5-(3-methylbutan-2-yl)-7-[5-(morpholin-4-yl)pyridin-2-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
-
3-amino-5-isobutyl-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
-
3-amino-5-sec-butyl-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
-
3-amino-7-[5-(1,1-dioxidothiomorpholin-4-yl)-1-methyl-1H-pyrazol-3-yl]-5-((2S)-3-methylbutan-2-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
-
3-amino-7-[5-(2-hydroxypropan-2-yl)-1-methyl-1H-pyrazol-3-yl]-5-((2S)-3-methylbutan-2-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
inhibits IL-23-induced IL-22 production in a rat pharmacodynamic assay, as well as inhibits IL-23 signaling in human peripheral blood mononuclear cell. It shows selectivity for IL-23 signaling inhibition against GMCSF, demonstrating the unique cytokine selectivity
3-[(3R,4R)-4-methyl-3-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl]-3-oxopropanenitrile
-
CP-690,550 JAK3-specific inhibitor
3-[3-[[4-(1,3-thiazol-2-yl)pyrimidin-2-yl]amino]-5-(trifluoromethyl)phenoxy]propan-1-ol
-
-
3-[[4-(1,3-thiazol-2-yl)pyrimidin-2-yl]amino]-5-(trifluoromethyl)phenol
-
-
4-(2,4-dichloro-5-methoxyanilino)-6-methoxy-7-[3-(4-methylpiperazin-1-yl)propoxy]quinoline-3-carbonitrile
-
inhibitor of Src and Abl
4-(2-(4-(2-((4-morpholinophenyl)amino)thieno[3,2-d]pyrimidin-4-yl)piperazin-1-yl)-2-oxoethyl)benzonitrile
100 nM, 17.6% inhibition. 28°C, pH not specified in the publication
4-(2-fluoro-3-(4-oxoquinazolin-3(4H)-yl)phenyl)-7-(2-hydroxypropan-2-yl)-9H-carbazole-1-carboxamide
-
4-(2-methyl-3-(1-oxoisoindolin-2-yl)phenyl)-7-(4-methylpiperazine-1-carbonyl)-9H-carbazole-1-carboxamide
-
4-(3-(4-fluorobenzamido)-2-methylphenyl)-7-(4-methylpiperazine-1-carbonyl)-9H-carbazole-1-carboxamide
-
4-(3-(4-fluorobenzamido)-2-methylphenyl)-7-(isopropylamino)-9H-carbazole-1-carboxamide
-
4-(3-(5-fluoro-4-oxoquinazolin-3(4H)-yl)-2-methylphenyl)-7-(2-hydroxypropan-2-yl)-9H-carbazole-1-carboxamide
-
4-(3-(5-fluoropicolinamido)-2-methylphenyl)-7-(4-methylpiperazine-1-carbonyl)-9H-carbazole-1-carboxamide
-
4-(3-(6-fluoro-1-oxoisoindolin-2-yl)-2-methylphenyl)-7-(2-hydroxypropan-2-yl)-9H-carbazole-1-carboxamide
-
4-(3-(6-fluoro-4-oxoquinazolin-3(4H)-yl)-2-methylphenyl)-7-(2-hydroxypropan-2-yl)-9H-carbazole-1-carboxamide
-
4-(3-(7-fluoro-4-oxoquinazolin-3(4H)-yl)-2-methylphenyl)-7-(2-hydroxypropan-2-yl)-9H-carbazole-1-carboxamide
-
4-(3-(8-fluoro-4-oxoquinazolin-3(4H)-yl)-2-methylphenyl)-7-(2-hydroxypropan-2-yl)-9H-carbazole-1-carboxamide
-
4-(4-(cyclopropylsulfonyl)piperazin-1-yl)-5-methyl-N-(4-morpholinophenyl)pyrimidin-2-amine
100 nM, 76.2% inhibition. 28°C, pH not specified in the publication
4-([4-[(5-chloro-1,3-benzodioxol-4-yl)amino]pyrimidin-2-yl]amino)benzenesulfonamide
-
-
4-([4-[(5-chloro-1,3-benzodioxol-4-yl)amino]pyrimidin-2-yl]amino)benzonitrile
-
-
4-amino-5-(4-chlorophenyl)-7-(t-butyl) pyrazolo[3,4-d]pyrimidine
-
-
4-amino-5-(4-chlorophenyl)-7-(t-butyl)pyrazolo[3,4-d]pyrimidine
4-amino-5-(4-chlorophenyl)-7-(tert-butyl)pyrazolo[3,4-d] pyrimidine
4-amino-5-(4-chlorophenyl)-7-(tert-butyl)pyrazolo[3,4-d]pyrimidine
4-amino-5-(4-methylphenyl)-7-(tert-butyl)pyrazolo[3,4-d] pyrimidine
4-amino-5-(4-methylphenyl)-7-(tert-butyl)pyrazolo[3,4-d]pyrimidine
4-amino-7-phenylpyrazolo[3,4-d] pyrimidine
i.e. pp3, inhibits Src family PTKs, slight inhibition of zebrafish egg/embryo development by Yes kinase inhibition
4-chloro-N-[5-[(3-chlorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
4-chloro-N-[5-[(3-fluorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
4-chloro-N-[5-[(4-fluorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
4-chloro-N-[5-[(4-methoxybenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
4-chloro-N-[5-[(4-nitrobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
4-fluoro-N-[5-[(3-fluorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
4-fluoro-N-[5-[(4-fluorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
4-fluoro-N-[5-[(4-methoxybenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
4-fluoro-N-[5-[(4-nitrobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
4-methyl-3-[[3-(pyrimidin-4-yl)pyridin-2-yl]amino]-N-[3-(trifluoromethyl)phenyl]benzamide
-
-
4-methyl-N-(3-methylphenyl)-6-(1,3-thiazol-2-yl)pyrimidin-2-amine
-
-
4-[4-([[3-tert-butyl-1-(quinolin-6-yl)-1H-pyrazol-5-yl]carbamoyl]amino)-3-fluorophenoxy]-N-methylpyridine-2-carboxamide
inhibitor binds to residues Arg386/Glu282 that isoform ABL1 uses to switch between inactive and active conformations. It potently inhibits both unphosphorylated and phosphorylated ABL1 by inducing a type II inactive conformation, and retains efficacy against the majority of clinically relevant chronic myeloid leukemia resistance mutants, including T315I. The compound inhibits isoform BCR-ABL1T315I-expressing cell lines, prolongs survival in mouse models of T315I-mutant chronic myeloid leukemia and B-lymphoblastic leukemia, and inhibits primary patient leukemia cells expressing mutation T315I in vitro and in vivo
5-methyl-4-(4-(methylsulfonyl)piperazin-1-yl)-N-(4-morpholinophenyl)pyrimidin-2-amine
100 nM, 1.0% inhibition. 28°C, pH not specified in the publication
7-(2-hydroxypropan-2-yl)-4-(2-methyl-3-(1-oxo-3,4-dihydroisoquinolin-2(1H)-yl)phenyl)-9H-carbazole-1-carboxamide
-
7-(2-hydroxypropan-2-yl)-4-(2-methyl-3-(1-oxoisoindolin-2-yl)phenyl)-9H-carbazole-1-carboxamide
-
7-(2-hydroxypropan-2-yl)-4-(2-methyl-3-(1-oxoisoquinolin-2(1H)-yl)phenyl)-9H-carbazole-1-carboxamide
-
7-(2-hydroxypropan-2-yl)-4-(3-(4-oxoquinazolin-3(4H)-yl)-phenyl)-9H-carbazole-1-carboxamide
-
7-(2-hydroxypropan-2-yl)-4-[2-methyl-3-(4-oxo-3,4-dihydroquinazolin-3-yl)phenyl]-9H-carbazole-1-carboxamide
BMS-935177
7-(hydroxymethyl)-4-(2-methyl-3-(4-oxoquinazolin-3(4H)-yl)phenyl)-9H-carbazole-1-carboxamide
-
8-(1-acetylpiperidin-4-yl)-2-((4-morpholinophenyl)amino)pteridin-7(8H)-one
100 nM, 3.5% inhibition. 28°C, pH not specified in the publication
8-methyl-emodin
-
inhibition of p56lck and c-Src
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(1-methylethoxy)-9H-purin-6-amine
-
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(1-methylethyl)-9H-purin-6-amine
-
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(1-methylpiperidin-4-yl)-9H-purin-6-amine
-
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(1H-imidazol-1-yl)-9H-purin-6-amine
-
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(2-methoxyethoxy)-9H-purin-6-amine
-
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(4-methylpiperazin-1-yl)-9H-purin-6-amine
-
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(pyrrolidin-3-yloxy)-9H-purin-6-amine
-
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-methoxy-9H-purin-6-amine
-
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-morpholin-4-yl-9H-purin-6-amine
-
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-pyrrolidin-1-yl-9H-purin-6-amine
-
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-9H-purin-6-amine
-
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dipropylphosphoryl)phenyl]-2-(1-methylethyl)-9H-purin-6-amine
-
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dipropylphosphoryl)phenyl]-9H-purin-6-amine
-
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N6-[4-(dimethylphosphoryl)phenyl]-N2,N2-dimethyl-9H-purine-2,6-diamine
-
9-[(E)-2-(2-chloro-6-methylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-9H-purin-6-amine
-
9-[(E)-2-(2-chlorophenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-9H-purin-6-amine
-
9-[(Z)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dipropylphosphoryl)phenyl]-2-(1-methylethyl)-9H-purin-6-amine
-
acacetin
-
inhibition of p56lck
AcpYEEI
ATP-phosphopeptide conjugate
ADP
-
competitive versus ATP, noncompetitive versus S1 peptide
AG-490
-
inhibits JAK2 tyrosine kinase
alsterpaullone
-
at 0.01 mM: 66% inhibition of CHK, 81% inhibition of LCK, and 10% inhibition of CSK
AMN107
-
a specific BCR-ABL tyrosine kinase inhibitor, Abl binding structure, in vivo inhibition study in chronic myeloid leukemia, CML, overview
apigenin
-
inhibition of p56lck
ATP-1,13-Trioxa-SA-phospho-Tyr-g-p-azido-Glu-Glu-Ile-OH
inhibition of SH2 domain tyrosine protein kinases
ATP-1,13-Trioxa-Suc-phospho-Tyr-Glu-Glu-Ile-OH
inhibition of SH2 domain tyrosine protein kinases
ATP-1,8-Diam-Suc-1,8-Diam-Suc-phospho-Tyr-Glu-Glu-Ile-OH
inhibition of SH2 domain tyrosine protein kinases
ATP-11-Aund-phospho-Tyr-Glu-Glu-Ile-OH
inhibition of SH2 domain tyrosine protein kinases
ATP-6-Ahex-phospho-Tyr-Glu-Glu-Ile-OH
inhibition of SH2 domain tyrosine protein kinases
ATP-8-Aoct-phospho-Tyr-Glu-Glu-Ile-OH
inhibition of SH2 domain tyrosine protein kinases
ATP-beta-Ala-phospho-Tyr-Glu-Glu-Ile-OH
inhibition of SH2 domain tyrosine protein kinases
AZ960
potent and selective ATP competitive inhibitor of JAK2 enzyme activity
Bcr protein
-
negative regulator
-
bengamide A
-
c-Src from bengamide A-treated cells retains its N-terminal methionine and suffers a decrease in N-terminal myristoylation, which is accompanied by a shift of its subcellular distribution from the plasma membrane to the cytosol, and decreased tyrosine kinase activities of c-Src both in vitro and in vivo and eventually delayed cell-cycle progression through G2/M, overview, bengamide A reduced tyrosine phosphorylation on a few proteins, and is not a general tyrosine kinase inhibitor
BGB324
i.e. Bemcentinib
-
BIRB-796
-
about 60% residual activity at 0.02 mM
bisindolylmaleimide I
-
blocks alboaggregin-A activation of Fyn
bistyrphostin
-
complete inhibition of TK-32
C-terminal Src kinase
-
i.e. CSK, an inhibitor which inactivates Src family of protein kinases by phosphorylating a consensus tyrosine YT near the C terminus, phosphorylated YT then intramolecularly binds to the enzyme's SH2 domain, pYT/SH2 interaction, together with binding between the SH2 kinase linker and the SH3 domain, stabilizes the enzyme in a closed inactive conformation, preparation of recombinant SH2 and SH3 domains by expression in Escherichia coli, overview
-
catenarin
-
i.e. 4-hydroxy-emodin, inhibition of p56lck and c-Src
caveolin
-
a non-catalytic inhibitor of SFKs, transient inhibition
-
CGP76030
-
growth-inhibitory in vivo
Chk
-
i.e. Csk-homologous kinase, a catalytic inhibitor of SFKs phosphorylating the regulatory tyrosine residue of SFK which leads to inhibition of SFK, Chk is also a 'non-catalytic inhibitor' binding directly to the SFK forming stable complexes and inhibiting it, mechanism, overview
-
chrysin
-
inhibition of p56lck
CMP6
-
i.e. 2-tert-butyl-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinoline-7-1, specific for JAK2, kinase domain binding structure and mechanism
CP690,550
-
targeting Jak3
Csk
-
i.e. C-terminal Src kinase, a catalytic inhibitor of SFKs phosphorylating the regulatory tyrosine residue of SFK which leads to inhibition of SFK, mechanism, overview
-
CSK-homologous kinase
-
i.e. CHK, an inhibitor which inactivates Src family of protein kinases by phosphorylating a consensus tyrosine YT near the C terminus, phosphorylated YT then intramolecularly binds to the enzyme's SH2 domain, pYT/SH2 interaction, together with binding between the SH2 kinase linker and the SH3 domain, stabilizes the enzyme in a closed inactive conformation, a second non-catalytic inhibitory mechanism involves tight binding of CHK to the enzyme's SFKs. The binding alone is sufficient to inhibit SFKs inhibition, preparation of recombinant SH2 and SH3 domains by expression in Escherichia coli, overview
-
cyclopropyl(4-(5-methyl-2-((4-morpholinophenyl)amino)pyrimidin-4-yl)piperazin-1-yl)methanone
100 nM, 77.0% inhibition. 28°C, pH not specified in the publication
damnacanthal
-
an anthraquinone, strong and selective inhibition of p56lck
datiscetin
-
inhibition of p56lck
DSA-1
-
about 10% residual activity at 0.02 mM
DSA-8
-
about 20% residual activity at 0.02 mM
emodic acid
-
inhibition of p56lck and c-Src
emodin derivatives
-
synthetic analogues, inhibition of p56lck and Src, overview
-
endocrocin
-
inhibition of p56lck and c-Src
F-actin
-
negative regulator
-
Fe3+
-
Lyn or Hck kinases in the unphosphorylated active state are significantly inhibited by Fe3+ ion
fisetin
-
inhibition of p56lck
flavone derivatives
-
inhibition of p56lck, overview
-
Fus1 protein
-
negative regulator
-
galangin
-
inhibition of p56lck
geldanamycin
-
indirect pharmacological inhibitor
genkwanin
-
inhibition of p56lck
Hg2+
-
at PO2 of about 20 mM
iclusig
-
potent inhibitor of Abl
INCB16562
-
selective, and orally bioavailable small-molecule inhibitor of JAK1 and JAK2 markedly selective over JAK3
INCB20
-
potently inhibits all members of the JAK family with a 100-1000fold selectivity for JAKs over more than 70 other kinases, potent and specific Pan-JAK inhibitor
-
indirubin-3'-monoxime
-
at 0.01 mM: 62% inhibition of CHK, 89% inhibition of LCK, but no inhibition of CSK
interdomain B
-
connects the enzyme's catalytic kinase domain with its SH2 domain, is responsible for regulatory autoinhibition of ZAP-70 involving Tyr315 and Tyr319, deletion of the interdomain B preserves enzyme function, the regulation mechanism is similar to receptor protein tyrosine kinase EphB2, EC 2.7.10.1, overview
-
interferon-gamma
-
enzyme inhibition in leukemic bone marrow cells
-
JAK-inhibitor I
40% JAK2 residual activity in the presence of 0.002 mM JAK-inhibitor I and 0.02 mM ATP
-
kaempferide
-
inhibition of p56lck
kaempferol
-
inhibition of p56lck
kaempferol-3-O-arabinoside
-
slight inhibition of p56lck
kaempferol-3-O-rhamnoside
-
slight inhibition of p56lck
kenpaullone
-
at 0.01 mM: 35% inhibition of CHK, 85% inhibition of LCK, and 14% inhibition of CSK
lavendustin A
-
PTK inhibitor, prevents the IP3 production in lemon seedlings in response to fungal attack and blocks the development of hypersensitive response
luteolin
-
inhibition of p56lck
MC25a
-
about 65% residual activity at 0.02 mM
methyl 2,5-dihydroxycinnamate
-
i.e. DHC, inhibition of Syk and Lyn
Mn2+
-
inhibitory above 1 mM
morin
-
inhibition of p56lck
myricetin
-
inhibition of p56lck
N,N-dimethyl-4-(5-methyl-2-((4-morpholinophenyl)amino)pyrimidin-4-yl)piperazine-1-carboxamide
100 nM, 63.4% inhibition. 28°C, pH not specified in the publication
N-(3,5-dimethoxyphenyl)-4-(1,3-thiazol-2-yl)pyrimidin-2-amine
-
-
N-(3,5-dimethylphenyl)-4-(1,3-thiazol-2-yl)pyrimidin-2-amine
-
-
N-(3,5-dimethylphenyl)-4-(4-methyl-1,3-thiazol-2-yl)pyrimidin-2-amine
-
-
N-(3,5-dimethylphenyl)-4-(5-methyl-1,3-thiazol-2-yl)pyrimidin-2-amine
-
-
N-(3-methylphenyl)-4-(1,3-thiazol-2-yl)pyrimidin-2-amine
-
-
N-(3-phenoxyphenyl)-4-(thiazol-2-yl)pyrimidin-2-amine
-
-
N-(3-[2-[4-(2-acetamidoethoxy)anilino]quinazolin-6-yl]-4-methylphenyl)-3-(trifluoromethyl)benzamide
-
-
N-(4-acetylphenyl)-1-(5-methyl-2-((4-morpholinophenyl) amino)pyrimidin-4-yl)piperidine-4-carboxamide
100 nM, 74.3% inhibition. 28°C, pH not specified in the publication
N-(4-acetylphenyl)-3-((5-methyl-2-((4-morpholinophenyl) amino)pyrimidin-4-yl)amino)azetidine-1-carboxamide
100 nM, 8.1% inhibition. 28°C, pH not specified in the publication
N-(4-acetylphenyl)-3-((5-methyl-2-((4-morpholinophenyl) amino)pyrimidin-4-yl)amino)pyrrolidine-1-carboxamide
100 nM, 69.3% inhibition. 28°C, pH not specified in the publication
N-(4-acetylphenyl)-4-((5-methyl-2-((4-morpholinophenyl) amino)pyrimidin-4-yl)amino)piperidine-1-carboxamide
100 nM, 80.5% inhibition. 28°C, pH not specified in the publication
N-(4-acetylphenyl)-4-(2-((4-morpholinophenyl)amino)-5-(trifluoromethyl)pyr-imidin-4-yl)piperazine-1-carboxamide
100 nM, 74.6% inhibition. 28°C, pH not specified in the publication
N-(4-acetylphenyl)-4-(2-((4-morpholinophenyl)amino)-5-nitropyrimidin-4-yl)piperazine-1-carboxamide
100 nM, 68.4% inhibition. 28°C, pH not specified in the publication
N-(4-acetylphenyl)-4-(2-((4-morpholinophenyl)amino)-7-oxopteridin-8(7H)-yl)piperidine-1-carboxamide
100 nM, 2.3% inhibition. 28°C, pH not specified in the publication
N-(4-acetylphenyl)-4-(2-((4-morpholinophenyl)amino)quinazolin-4-yl)piperazine-1-carboxamide
100 nM, 3.2% inhibition. 28°C, pH not specified in the publication
N-(4-acetylphenyl)-4-(5-amino-2-((4-morpholinophenyl)amino) pyrimidin-4-yl)piperazine-1-carboxamide
100 nM, 22.8% inhibition. 28°C, pH not specified in the publication
N-(4-acetylphenyl)-4-(5-chloro-2-((4-morpholinophenyl)amino) pyrimidin-4-yl)piperazine-1-carboxamide
100 nM, 99.4% inhibition. 28°C, pH not specified in the publication
N-(4-acetylphenyl)-4-(5-fluoro-2-((4-morpholinophenyl)amino) pyrimidin-4-yl)piperazine-1-carboxamide
100 nM, 93.5% inhibition. 28°C, pH not specified in the publication
N-(4-acetylphenyl)-4-(5-methyl-2-((4-morpholinophenyl) amino)pyrimidin-4-yl)piperazine-1-sulfonamide
100 nM, 82.4 % inhibition. 28°C, pH not specified in the publication
N-(4-acetylphenyl)-4-(5-methyl-2-((4-morpholinophenyl)amino)pyrimidin-4-yl)piperazine-1-carboxamide
2.9 nM, 81.8% inhibition. 28°C, pH not specified in the publication
N-(4-acetylphenyl)-4-(6-methyl-2-((4-morpholinophenyl)amino)pyrimidin-4-yl)piperazine-1-carboxamide
100 nM, 15.6% inhibition. 28°C, pH not specified in the publication
N-(4-acetylphenyl)-4-[2-[4-(morpholin-4-yl)anilino]pyrimidin-4-yl]piperazine-1-carboxamide
27 nM, 86.7% inhibition. 28°C, pH not specified in the publication
N-(4-cyanophenyl)-1-(5-methyl-2-((4-morpholinophenyl) amino)pyrimidin-4-yl)piperidine-4-carboxamide
100 nM, 72.8% inhibition. 28°C, pH not specified in the publication
N-(4-cyanophenyl)-4-(2-((4-morpholinophenyl)amino)quinazolin-4-yl)piperazine-1-carboxamide
100 nM, 9.7% inhibition. 28°C, pH not specified in the publication
N-(4-cyanophenyl)-4-(5-methyl-2-((4-morpholinophenyl)amino)pyrimidin-4-yl)piperazine-1-carboxamide
100 nM, 88.5% inhibition. 28°C, pH not specified in the publication
N-(4-cyanophenyl)-4-(6-methyl-2-((4-morpholinophenyl)amino)pyrimidin-4-yl)piperazine-1-carboxamide
100 nM, 8.9% inhibition. 28°C, pH not specified in the publication
N-(4-methyl-3-[[3-(pyrimidin-4-yl)pyridin-2-yl]amino]phenyl)-3-(trifluoromethyl)benzamide
-
-
N-(5-chloro-1,3-benzodioxol-4-yl)-6-methoxy-7-(3-piperidin-1-ylpropoxy)quinazolin-4-amine
-
-
N-(5-chloro-1,3-benzodioxol-4-yl)-N'-(3,4,5-trimethoxyphenyl)-1,3,5-triazine-2,4-diamine
-
-
N-(5-chloro-1,3-benzodioxol-4-yl)-N'-(3,4,5-trimethoxyphenyl)pyrimidine-4,6-diamine
-
-
N-([[N2-(1-[4-[3-(4-[6-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]-2-methylpyrimidin-4-yl]piperazin-1-yl)-3-oxopropyl]-1H-1,2,3-triazol-1-yl]-28,32-dioxo-3,6,9,12,15,18,21,24,30-nonaoxa-27-azadotriacontan-32-yl)-L-glutaminyl]amino][4-(phosphonooxy)phenyl]acetyl)-L-alpha-glutamyl-alpha-glutamyl-L-isoleucinamide
-
N-tert-butyl-3-([5-methyl-2-[(4-piperazin-1-ylphenyl)amino]pyrimidin-4-yl]amino)benzenesulfonamide
-
TG101209
N-tert-butyl-3-[(5-methyl-2-[[4-(2-pyrrolidin-1-ylethoxy)phenyl]amino]pyrimidin-4-yl)amino]benzenesulfonamide
-
TG101348, JAK2-specific inhibitor
N-[3-([3-[4-(4-methoxyanilino)-1,3,5-triazin-2-yl]pyridin-2-yl]amino)-4-methylphenyl]-3-(trifluoromethyl)benzamide
-
-
N-[3-methoxy-5-(trifluoromethyl)phenyl]-4-(1,3-thiazol-2-yl)pyrimidin-2-amine
-
-
N-[3-methoxy-5-(trifluoromethyl)phenyl]-4-(5-methyl-1,3-thiazol-2-yl)pyrimidin-2-amine
-
-
N-[3-methyl-5-(trifluoromethyl)phenyl]-4-(1,3-thiazol-2-yl)pyrimidin-2-amine
-
-
N-[3-[2-(cyclopropylamino)quinazolin-6-yl]-4-methylphenyl]-3-(trifluoromethyl)benzamide
-
-
N-[4-(dimethylphosphoryl)phenyl]-9-[(E)-2-(1H-indazol-4-yl)ethenyl]-9H-purin-6-amine
-
N-[4-(dimethylphosphoryl)phenyl]-9-[(E)-2-(1H-indol-4-yl)ethenyl]-9H-purin-6-amine
-
N-[4-(dimethylphosphoryl)phenyl]-9-[(E)-2-(5-methyl-1H-indazol-4-yl)ethenyl]-9H-purin-6-amine
-
N-[4-(dipropylphosphoryl)phenyl]-2-(1-methylethyl)-9-[(E)-2-phenylethenyl]-9H-purin-6-amine
-
N-[4-(dipropylphosphoryl)phenyl]-2-(1-methylethyl)-9-[(Z)-2-phenylethenyl]-9H-purin-6-amine
-
N-[4-methyl-3-([3-[2-(methylamino)pyrimidin-4-yl]pyridin-2-yl]amino)phenyl]-3-(trifluoromethyl)benzamide
-
-
N-[4-methyl-3-([3-[6-(methylamino)pyrimidin-4-yl]pyridin-2-yl]amino)phenyl]-3-(trifluoromethyl)benzamide
-
-
N-[4-[4-amino-1-(propan-2-yl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl]phenyl]-N'-[3-(trifluoromethyl)phenyl]urea
-
-
N-[5-(benzylsulfanyl)-1,3,4-thiadiazol-2-yl]-2-chlorobenzamide
-
N-[5-(benzylsulfanyl)-1,3,4-thiadiazol-2-yl]-4-chlorobenzamide
-
N-[5-[(3-chlorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]-4-fluorobenzamide
-
N-[5-[(4-bromobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]-2-chlorobenzamide
-
N-[5-[(4-bromobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]-4-chlorobenzamide
-
N-[5-[(4-bromobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]-4-fluorobenzamide
-
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(2-chlorophenyl)pyrimidine-2,4-diamine
-
-
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(2-fluorophenyl)pyrimidine-2,4-diamine
-
-
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(2-methoxyphenyl)pyrimidine-2,4-diamine
-
-
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(2-methylphenyl)pyrimidine-2,4-diamine
-
-
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(2-morpholin-4-ylphenyl)pyrimidine-2,4-diamine
-
-
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(3,4,5-trimethoxyphenyl)pyrimidine-2,4-diamine
-
-
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(3-chlorophenyl)pyrimidine-2,4-diamine
-
-
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(3-fluorophenyl)pyrimidine-2,4-diamine
-
-
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(3-methoxyphenyl)pyrimidine-2,4-diamine
-
-
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(3-methylphenyl)pyrimidine-2,4-diamine
-
-
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(3-morpholin-4-ylphenyl)pyrimidine-2,4-diamine
-
-
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(4-chlorophenyl)pyrimidine-2,4-diamine
-
-
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(4-fluorophenyl)pyrimidine-2,4-diamine
-
-
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(4-methoxyphenyl)pyrimidine-2,4-diamine
-
-
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(4-methylphenyl)pyrimidine-2,4-diamine
-
-
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(4-morpholin-4-ylphenyl)pyrimidine-2,4-diamine
-
-
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-phenylpyrimidine-2,4-diamine
-
-
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-[2-(methylsulfonyl)phenyl]pyrimidine-2,4-diamine
-
-
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-[3-(methylsulfonyl)phenyl]pyrimidine-2,4-diamine
-
-
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-[4-(methylsulfonyl)phenyl]pyrimidine-2,4-diamine
-
-
N6-Dimethylaminopurine
-
unspecific inhibitor of protein kinases
nevadensin
-
inhibition of p56lck
NS-187
-
a specific dual ABL-LYN inhibitor
ON012380
-
inhibits wild-type and mutant Abls, substrate-competitive, ATP-incompetitive
p-fluorosulfonylbenzoyl 5'-adenosine
inactivates tyrosine protein kinase activity of p60src by reacting with lysine 295
paeciloquinone A
-
inhibition of p56lck and c-Src
Paeciloquinone B
-
inhibition of p56lck and c-Src
paeciloquinone C
-
inhibition of p56lck and c-Src
paeciloquinone D
-
inhibition of p56lck and c-Src
PAG protein
-
negative regulator
-
phosphoinositide
-
negative regulator
protein tyrosine phosphatases
-
e.g. T-cell protein tyrosine phosphatase, catalytic inhibitor of SFKs dephosphorylating the autoactivation tyrosine residue of SFK which leads to inhibition of SFK
-
purpurin
-
inhibition of p56lck and c-Src
purvalanol
-
at 0.01 mM: 22% inhibition of CHK, 80% inhibition of LCK and CSK
Pyk2-specific siRNA
-
-
-
quercetin
-
inhibition of p56lck
RACK1
-
a non-catalytic inhibitor of SFKs, transient inhibition
-
rebastinib
-
potent inhibitor of Abl
resokaempferol
-
inhibition of p56lck
resveratrol
-
inhibition of p56lck
RNAi
knockdown of Btk results in decreased tumor necrosis factor-alpha
-
saracatinib
-
inhibitor of Src and Abl
sorafenib
-
about 30% residual activity at 0.02 mM
Src kinase inhibitor-1
-
i.e. SKI-1, a 4-anilinoquinazoline, moderate inhibition in vitro and vivo
-
stilbene derivatives
-
inhibition of p56lck, overview
-
syringetin
-
inhibition of p56lck
T47
-
57% inhibition of Syk at 0.1 mM
tyrphostin 25
-
p38 MAP kinase inhibitor SB203580 and protein tyrosine kinase inhibitor tyrphostin 25 combined can be used for inhibition of matrix metalloproteinase-9 expression, overview
tyrphostin A25
-
broad-spectrum PTK inhibitor, slight inhibition of Src
VX-680
-
about 5% residual activity at 0.02 mM
WASP
-
a non-catalytic inhibitor of SFKs, e.g. c-Src, mechanism, transient inhibition
-
[2-(2-[[3-methoxy-5-(trifluoromethyl)phenyl]amino]pyrimidin-4-yl)-1,3-thiazol-4-yl]methanol
-
-
[2-(2-[[3-methyl-5-(trifluoromethyl)phenyl]amino]pyrimidin-4-yl)-1,3-thiazol-4-yl]methanol
-
-
4-amino-5-(4-chlorophenyl)-7-(t-butyl)pyrazolo[3,4-d]pyrimidine
PP2, AG-1897
4-amino-5-(4-chlorophenyl)-7-(t-butyl)pyrazolo[3,4-d]pyrimidine
-
PP2, AG-1897
4-amino-5-(4-chlorophenyl)-7-(t-butyl)pyrazolo[3,4-d]pyrimidine
-
PP2
4-amino-5-(4-chlorophenyl)-7-(t-butyl)pyrazolo[3,4-d]pyrimidine
PP2
4-amino-5-(4-chlorophenyl)-7-(tert-butyl)pyrazolo[3,4-d] pyrimidine
i.e. pp2, inhibits Src family PTKs, inhibition of zebrafish egg/embryo development by Yes kinase inhibition
4-amino-5-(4-chlorophenyl)-7-(tert-butyl)pyrazolo[3,4-d] pyrimidine
-
i.e. pp2, inhibits Src family PTKs
4-amino-5-(4-chlorophenyl)-7-(tert-butyl)pyrazolo[3,4-d] pyrimidine
-
i.e. pp2, synthetic inhibitor, inhibits SFKs by binding competitively to the ATP-binding site
4-amino-5-(4-chlorophenyl)-7-(tert-butyl)pyrazolo[3,4-d] pyrimidine
-
i.e. pp2, inhibits Src family PTKs
4-amino-5-(4-chlorophenyl)-7-(tert-butyl)pyrazolo[3,4-d] pyrimidine
-
i.e. pp2, inhibition of Csk involves Thr265, no inhibition of Chk
4-amino-5-(4-chlorophenyl)-7-(tert-butyl)pyrazolo[3,4-d] pyrimidine
-
i.e. pp2, ihibits Src family PTKs
4-amino-5-(4-chlorophenyl)-7-(tert-butyl)pyrazolo[3,4-d] pyrimidine
-
-
4-amino-5-(4-chlorophenyl)-7-(tert-butyl)pyrazolo[3,4-d] pyrimidine
-
i.e. PP2, abolishes the hypoxia-induced inhibition of Kv1.3 channels in primaryhumanT lymphocytes
4-amino-5-(4-chlorophenyl)-7-(tert-butyl)pyrazolo[3,4-d] pyrimidine
-
i.e. pp2, inhibits Src family PTKs
4-amino-5-(4-chlorophenyl)-7-(tert-butyl)pyrazolo[3,4-d] pyrimidine
-
i.e. pp2, broad spectrum SFK inhibitor, competitive to ATP, in vitro and in vivo
4-amino-5-(4-chlorophenyl)-7-(tert-butyl)pyrazolo[3,4-d] pyrimidine
-
-
4-amino-5-(4-chlorophenyl)-7-(tert-butyl)pyrazolo[3,4-d] pyrimidine
-
i.e. pp2, inhibits Src family PTKs
4-amino-5-(4-chlorophenyl)-7-(tert-butyl)pyrazolo[3,4-d] pyrimidine
-
enzyme inhibition prevents internalization of the organism into host cells
4-amino-5-(4-chlorophenyl)-7-(tert-butyl)pyrazolo[3,4-d] pyrimidine
-
i.e. pp2, inhibits Src family PTKs
4-amino-5-(4-chlorophenyl)-7-(tert-butyl)pyrazolo[3,4-d] pyrimidine
-
-
4-amino-5-(4-chlorophenyl)-7-(tert-butyl)pyrazolo[3,4-d]pyrimidine
-
i.e. pp2, Lck inhibitor
4-amino-5-(4-chlorophenyl)-7-(tert-butyl)pyrazolo[3,4-d]pyrimidine
-
i.e. pp2, inhibits Src family members like Lyn, no inhibition of Syk
4-amino-5-(4-chlorophenyl)-7-(tert-butyl)pyrazolo[3,4-d]pyrimidine
-
application completely abolishes thrombin-induced non-capacitative cation entry into platelets, a Ca2+ entry pathway that is independent of Ca2+ store depletion. Src family tyrosine kinase activation is a required step in non-capacitative cation entry activation
4-amino-5-(4-chlorophenyl)-7-(tert-butyl)pyrazolo[3,4-d]pyrimidine
-
i.e. PP2, inhibits Src
4-amino-5-(4-chlorophenyl)-7-(tert-butyl)pyrazolo[3,4-d]pyrimidine
-
selective Src-kinase inhibitors 4-amino-5-(4-methylphenyl)-7-(tert-butyl)pyrazolo[3,4-d]pyrimidine and 4-amino-5-(4-chlorophenyl)-7-(tert-butyl)pyrazolo[3,4-d]pyrimidine, at 5 microM, attenuate acetylcholine-induced ionic currents and intracellular Ca2+ ion concentration transients in major pelvic ganglion neurons
4-amino-5-(4-methylphenyl)-7-(tert-butyl)pyrazolo[3,4-d] pyrimidine
-
i.e. pp1, synthetic inhibitor, inhibits SFKs by binding competitively to the ATP-binding site
4-amino-5-(4-methylphenyl)-7-(tert-butyl)pyrazolo[3,4-d] pyrimidine
-
i.e. pp1, inhibits Src family PTKs
4-amino-5-(4-methylphenyl)-7-(tert-butyl)pyrazolo[3,4-d] pyrimidine
-
-
4-amino-5-(4-methylphenyl)-7-(tert-butyl)pyrazolo[3,4-d] pyrimidine
-
-
4-amino-5-(4-methylphenyl)-7-(tert-butyl)pyrazolo[3,4-d] pyrimidine
-
-
4-amino-5-(4-methylphenyl)-7-(tert-butyl)pyrazolo[3,4-d]pyrimidine
-
i.e. pp1, inhibits Src family members like Lyn, no inhibition of Syk
4-amino-5-(4-methylphenyl)-7-(tert-butyl)pyrazolo[3,4-d]pyrimidine
-
selective Src-kinase inhibitors 4-amino-5-(4-methylphenyl)-7-(tert-butyl)pyrazolo[3,4-d]pyrimidine and 4-amino-5-(4-chlorophenyl)-7-(tert-butyl)pyrazolo[3,4-d]pyrimidine, at 5 microM, attenuate acetylcholine-induced ionic currents and intracellular Ca2+ ion concentration transients in major pelvic ganglion neurons
A-419259
-
-
A-419259
-
high inhibition of SFKs
AG490
-
-
AG490
-
potent JAK2 inhibitor
AP23464
-
ineffective against Abl mutant T315I, but inhibitory against imatinib-resistant mutants M351I, E255K, Q252H, and Y253F, and activation loop mutant H396P
AZD-1480
-
Jak2 inhibitor
AZD-1480
-
Jak2 inhibitor
AZM 475271
-
-
bosutinib
i.e. SKI-606, a dual Src/Abl inhibitor
bosutinib
-
previously SKI-606, inhibits ABL1
bosutinib
two distinct chemical compounds are currently being sold under the name bosutinib, spectroscopic and structural characterizations of both
bosutinib
-
previously SKI-606, inhibits ABL1
CGP 76030
-
-
CGP 77675
-
-
CP-690 550
-
Jak3 and Jak2 inhibitor
CP-690 550
-
Jak3 and Jak2 inhibitor
CP-690,550
-
orally active JAK inhibitor that potently inhibits JAK3
CP-690,550
-
has nanomolar potency in in vitro JAK2 and JAK3 kinase assays
CP-690,550
-
JAK3-specific inhibitor
CP-690,550
-
has nanomolar potency in in vitro JAK2 and JAK3 kinase assays
curcumin
-
inhibits the JAK-STAT signaling cascade via activation of SHP-2, a SH2 domain-containing phosphatase, and increase in JAK-SHP-2 interaction contributing to anti-inflammatory activity in the brain, suppresses STAT-responsive inflammatory gene expression
curcumin
-
downregulates and inhibits tyrosine kinase Syk, which leads to inhibition of Akt, in lymphoma cells, curcumin causes growth inhibition of B lymphoma, mechanism, overview
curcumin
-
downregulates and inhibits tyrosine kinase Syk, which leads to inhibition of Akt, in lymphoma cells, curcumin causes growth inhibition of B lymphoma, mechanism, overview
dasatinib
response of enzymes with BCR-ABL kinase domain in in vivo study are similar for patients with different mutations, except for T315I, which is more resistant
dasatinib
-
i.e. BMS-354825, Abl binding structure, in vivo inhibition study in chronic myeloid leukemia, CML, overview
dasatinib
-
i.e. BMS-354825, a Bcr-Abl inhibitor, used for the treatment of imatinib-resistant chronic myelogenous leukemia, inhibits Abl and Src kinases, and the Tec kinases Btk at Th474 and Tec at Thr442, but not Itk, the mutant BtkT474I ans TecT442I are resistant to dasatinib, while mutantion of the insensitive wild-type Itk to ItkF435T renders the enzyme sensitive to dasatinib, overview, autophosphorylation of Btk at Tyr223 is inhibited only by dasatinib but not by imatinib or nilotinib
dasatinib
-
Jak2 inhibitor, at high doses (0.001 mM), dasatinib can inhibit Jak2 activity in vitro
dasatinib
-
potent ABL1 inhibitor
dasatinib
-
about 3% residual activity at 0.02 mM
dasatinib
-
Jak2 inhibitor, at high doses (0.001 mM), dasatinib can inhibit Jak2 activity in vitro
dasatinib
-
potent ABL1 inhibitor
emodin
-
inhibition of p56lck and c-Src
emodin
-
i.e. 6-methyl-1,3,8-trihydroxyanthraquinone, Lck inhibitor
genistein
-
protein tyrosine kinase inhibitor
genistein
-
broad-spectrum PTK inhibitor, increases volume-sensitive chloride current in atrial myocytes, is antagonized by pretreatment with VO43-
genistein
-
broad spectrum PTK inhibitor
genistein
-
isoflavone, inhibits PTKs, and reversibly inhibits voltage-dependent transient outward and rectifier inward K+-currents in myocytes, overview
Gleevec
also known as STI-571 or imatinib
Gleevec
also known as STI-571 or imatinib
Gleevec
also known as STI-571 or imatinib
ibrutinib
-
imatinib
response of enzymes with BCR-ABL kinase domain in in vivo study are similar for patients with different mutations, except for T315I, which is more resistant
imatinib
-
i.e. STI-571, Abl binding structure, in vivo inhibition study in chronic myeloid leukemia, CML, overview
imatinib
-
inhibits ABL1autophosphorylation as well as substrate phosphorylation
imatinib
-
a c-Abl-family kinase inhibitor, prevents the phosphorylation of substrate parkin, maintaining parkin in a catalytically active and protective state. The protective effects require parkin
imatinib
-
about 80% residual activity at 0.02 mM
imatinib
-
inhibits ABL1autophosphorylation as well as substrate phosphorylation
imatinib mesylate
-
2-phenylaminopyrimidine derivate, i.e. CGP-57148, inhibits BCR/ABL kinase, used in antityrosine kinase therapy of myeloid leukemia
imatinib mesylate
-
Gleevec
INCB018424
Jak2 inhibitor
INCB018424
-
Jak2 inhibitor
INCB018424
-
Jak2 inhibitor
INCB18424
-
Incyte
INCB18424
-
targeting Jak1/2
INNO-406
-
previously NS-187, inhibits ABL1
INNO-406
-
previously NS-187, inhibits ABL1
ITF2357
-
Jak2 inhibitor
lestaurtinib
-
Jak2 inhibitor
lestaurtinib
-
formerly CEP701, JAK2 inhibitor
lestaurtinib
-
Jak2 inhibitor
lestaurtinib
-
formerly CEP701, JAK2 inhibitor
LFM-A13
-
significantly impairs CXCL12-induced human B lymphoma cell line, and blocks Akt activation, homing of transferred B cells to peripheral lymph nodes is impaired, LFM-A13 significantly reduces the CXCL12-induced increases in Ca2+, overview
LFM-A13
-
significantly impairs CXCL12-induced mouse B cell chemotaxis, and blocks Akt activation, homing of transferred B cells to peripheral lymph nodes is impaired, LFM-A13 significantly reduces the CXCL12-induced increases in Ca2+, overview
LS104
-
Jak2 inhibitor
LS104
i.e. [(E,E)-2-(benzylaminocarbonyl)-3-(3,4-dihydroxystyryl)acrylonitrite], non-ATP-competitive small-molecule inhibitor of JAK2, 20% residual activity of mutant V617F in the resence of 0.02 mM LS104 and 0.02 mM ATP
M 475271
-
-
MK-0457
-
Jak2 inhibitor
nilotinib
response of enzymes with BCR-ABL kinase domain in in vivo study are similar for patients with different mutations, except for T315I, which is more resistant
nilotinib
-
potent ABL1 inhibitor
nilotinib
-
about 70% residual activity at 0.02 mM
nilotinib
-
potent ABL1 inhibitor
PD166326
-
-
peroxiredoxin 1
-
inhibits ABL1 intracellularly
-
peroxiredoxin 1
-
inhibits ABL1 intracellularly
-
piceatannol
-
inhibition of p56lck
piceatannol
-
Syk kinase inhibitor
piceatannol
-
Syk inhibitor in vitro and in vivo
PIP2
-
inhibits ABL1 intracellularly
PIP2
-
inhibits ABL1 intracellularly
PNU156804
-
Jak3 inhibitor
PNU156804
-
Jak3 inhibitor
PP1
-
-
PP1
-
growth-inhibitory in vivo
PP2
-
-
SB1518
-
Jak2 inhibitor
siRNA
-
-
-
SKI-606
-
-
SKI-606
-
cytotoxic inhibitor of BCR-ABL
staurosporine
-
unspecific inhibitor of protein kinases
staurosporine
-
i.e. ST, inhibition of Syk and Lyn, IC50 for Syk is 0.008 mM
staurosporine
-
competitive versus ATP, noncompetitive versus S1 peptide
SU-6656
-
-
SU6656
-
-
SU6656
-
more specific for Yes kinase than for other SFKs
TG101209
Jak2 inhibitor
TG101209
-
Jak2 inhibitor
TG101209
-
Jak2 inhibitor
TG101348
-
Jak2 inhibitor
TG101348
-
JAK2-specific inhibitor
TG101348
-
Jak2 inhibitor
tyrphostin A23
-
broad-spectrum PTK inhibitor, slight inhibition of Src
tyrphostin A23
-
inhibits PTKs
tyrphostin AG490
-
Jak3 inhibitor
tyrphostin AG490
-
Jak3 inhibitor
WHI-P131
-
Jak3 inhibitor
WHI-P131
-
Jak3 inhibitor
WHI-P154
-
Jak3 inhibitor
WHI-P154
-
Jak3 inhibitor
XL019
-
Exelixis
additional information
-
no inhibition by daidzein
-
additional information
completely inhibited by an excess of substrate peptide
-
additional information
Abl-SH3 domain is implicated in negative regulation of the Abl kinase by mediating protein-protein interactions
-
additional information
-
no or poor inhibition of CHK1, LCK, and CSK by roscovitine
-
additional information
-
enzyme interaction studies using inhibitory antibodies, overview
-
additional information
-
SFKs are regulated involving autophosphorylation for activation and inhibition by diverse endogenous catalytic and non-catalytic inhibitors acting directly or via down-regulation of SFKs, recognition and mechanisms involving Csk and Chk, overview
-
additional information
synthesis, inhibitory potency, and mechanism of ATP-SH2-domain-derived phosphopeptide conjugates with short or long linkers binding at the ATP-binding site, structure-activity-relationship, overview
-
additional information
-
epidermal growth factor receptor EGFR induces Syk inhibition
-
additional information
-
daidzein is no inhibitor of PTKs, no direct Src kinase inhibition by tyrphostin AG17, tyrphosptin AG879 and genistein
-
additional information
-
analysis of inhibitory potential and cytotoxic effects of a large number of plant-derived secondary metabolites on PTKs and human tumor cell lines, respectively, overview
-
additional information
-
regulation of Lck by phosphorylation at Tyr505 by C-terminal Scr protein-tyrosine kinase which inhibits the enzyme
-
additional information
-
effects of inhibitors in vivo in SS cells on K-Cl cotransport, overview
-
additional information
-
inhibition of the Src phosphorylation by peptides mimicking the substrate binding site, overview
-
additional information
-
enzyme is cleaved by several proteases such as thrombin
-
additional information
development and evaluation of tyrosine kinase inhibitors
-
additional information
-
development and evaluation of tyrosine kinase inhibitors
-
additional information
-
inhibition of epidermal growth factor stimulation inhibits fyn enzyme activity
-
additional information
-
inhibition evaluation study using Src family tyrosine kinase inhibitors and Abl tyrosine kinase, overview
-
additional information
-
no inhibition by 4-amino-7-phenylpyrazolo[3,4-d] pyrimidine, i.e. PP3
-
additional information
-
c-Abl is inactivated by interactions made by its SH3 and SH2 domains with the distal surface of the kinase domain, a critical N-terminal cap segment, phosphorylated on a serine residue that interacts with the connector between the SH3 and SH2 domains, buttresses the SH3-SH2 substructure in the autoinhibited state and locks it onto the distal surface of the kinase domain, overview
-
additional information
-
pY213 phosphopeptide of Abi1 inhibits c-Abl kinase activity by a noncompetitive mechanism
-
additional information
-
c-Abl is downregulated in part by intramolecular interactions that provide autoinhibitory kinase effects
-
additional information
-
phosphorylation of Y527 leads to the inactivation of c-Src, negative regulation
-
additional information
-
ABL1 is autoinhibited in an intramolecular fashion that is similar to SRC kinases, where the SH3 domain is engaged with a single proline residue in the spacer region between the SRC homology 2 and tyrosine kinase domains
-
additional information
JAK2 is not inhibited by STI571
-
additional information
-
exposure of BE(2)-C cells to the heavy metals Cd2+ and Hg2+ and to rotenone inhibits interleukin-6, interferon-gamma and ciliary neurotrophic factor-mediated Jak/STAT signaling, reduces Jak1 and Jak2 autophosphorylation and induces Jak tyrosine nitration by mitochondrial disruption. Identical exposure of HepG2 hepatoma cells produces no inhibition of these cytokine responses.
-
additional information
use of the DNA repair enzyme O6-alkylguanine-DNA alkyltransferase AGT to display an ATP-competitive inhibitor and a ligand that targets a secondary binding domain. Systematic analysis of ATP-competitive inhibitors with varying linker lengths reveals that isoforms SRC and ABL have differential sensitivities to ligand presentation. Generation of bivalent constructs that contain ligands with differential affinities for the ATP-binding sites and SH3 domains of SRC and ABL demonstrates the modular nature of inhibitors based on the O6-alkylguanine-DNA alkyltransferase scaffold. The interaction between the SH3 domain ligand and the kinase SH3 domain is the major selectivity determinant amongst closely-related tyrosine kinases; use of the DNA repair enzyme O6-alkylguanine-DNA alkyltransferase AGT to display an ATP-competitive inhibitor and a ligand that targets a secondary binding domain. Systematic analysis of ATP-competitive inhibitors with varying linker lengths reveals that isoforms SRC and ABL have differential sensitivities to ligand presentation. Generation of bivalent constructs that contain ligands with differential affinities for the ATP-binding sites and SH3 domains of SRC and ABL demonstrates the modular nature of inhibitors based on the O6-alkylguanine-DNA alkyltransferase scaffold. The interaction between the SH3 domain ligand and the kinase SH3 domain is the major selectivity determinant amongst closely-related tyrosine kinases
-
additional information
use of the DNA repair enzyme O6-alkylguanine-DNA alkyltransferase AGT to display an ATP-competitive inhibitor and a ligand that targets a secondary binding domain. Systematic analysis of ATP-competitive inhibitors with varying linker lengths reveals that isoforms SRC and ABL have differential sensitivities to ligand presentation. Generation of bivalent constructs that contain ligands with differential affinities for the ATP-binding sites and SH3 domains of SRC and ABL demonstrates the modular nature of inhibitors based on the O6-alkylguanine-DNA alkyltransferase scaffold. The interaction between the SH3 domain ligand and the kinase SH3 domain is the major selectivity determinant amongst closely-related tyrosine kinases; use of the DNA repair enzyme O6-alkylguanine-DNA alkyltransferase AGT to display an ATP-competitive inhibitor and a ligand that targets a secondary binding domain. Systematic analysis of ATP-competitive inhibitors with varying linker lengths reveals that isoforms SRC and ABL have differential sensitivities to ligand presentation. Generation of bivalent constructs that contain ligands with differential affinities for the ATP-binding sites and SH3 domains of SRC and ABL demonstrates the modular nature of inhibitors based on the O6-alkylguanine-DNA alkyltransferase scaffold. The interaction between the SH3 domain ligand and the kinase SH3 domain is the major selectivity determinant amongst closely-related tyrosine kinases
-
additional information
a general methodology is developed to produce bivalent kinase inhibitors for c-Src that interact with the SH2 and ATP binding pockets
-
additional information
a general methodology is developed to produce bivalent kinase inhibitors for c-Src that interact with the SH2 and ATP binding pockets
-
additional information
a general methodology is developed to produce bivalent kinase inhibitors for c-Src that interact with the SH2 and ATP binding pockets
-
additional information
a general methodology is developed to produce bivalent kinase inhibitors for c-Src that interact with the SH2 and ATP binding pockets
-
additional information
a general methodology is developed to produce bivalent kinase inhibitors for c-Src that interact with the SH2 and ATP binding pockets
-
additional information
a general methodology is developed to produce bivalent kinase inhibitors for c-Src that interact with the SH2 and ATP binding pockets
-
additional information
a general methodology is developed to produce bivalent kinase inhibitors for c-Src that interact with the SH2 and ATP binding pockets
-
additional information
development of potent inhibitors of receptor tyrosine kinases by ligand-based drug design and target-biased phenotypic screening
-
additional information
-
phosphorylation of Tyr508 in Lyn inhibits activity of the enzyme
-
additional information
-
ABL1 is autoinhibited in an intramolecular fashion that is similar to SRC kinases, where the SH3 domain is engaged with a single proline residue in the spacer region between the SRC homology 2 and tyrosine kinase domains
-
additional information
-
no inhibition of Src with pp3, i.e. 4-amino-7-phenylpyrazolo[3,4-d] pyrimidine
-
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0.0029 - 0.0218
1-(4-[6-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]-2-methylpyrimidin-4-yl]piperazin-1-yl)-3-(1-nonadecyl-1H-1,2,3-triazol-4-yl)propan-1-one
0.00107
1-(4-[[6-amino-5-(4-phenoxybenzoyl)pyrimidin-4-yl]amino]piperidin-1-yl)prop-2-en-1-one
Homo sapiens
pH and temperature not specified in the publication
0.0018
1-[(3R)-3-[[6-amino-5-(4-ethoxybenzoyl)pyrimidin-4-yl]amino]piperidin-1-yl]prop-2-en-1-one
Homo sapiens
pH and temperature not specified in the publication
0.00132
1-[4-[6-amino-5-(4-ethoxybenzoyl)pyrimidin-4-yl]piperazin-1-yl]prop-2-en-1-one
Homo sapiens
pH and temperature not specified in the publication
0.00088
1-[4-[6-amino-5-(4-phenoxybenzoyl)pyrimidin-4-yl]piperazin-1-yl]prop-2-en-1-one
Homo sapiens
pH and temperature not specified in the publication
0.0355
2-([4-[(5-chloro-1,3-benzodioxol-4-yl)amino]pyrimidin-2-yl]amino)benzenesulfonamide
Mammalia
-
-
0.02049
2-([4-[(5-chloro-1,3-benzodioxol-4-yl)amino]pyrimidin-2-yl]amino)benzonitrile
Mammalia
-
-
0.00000129 - 0.0000323
2-cyclopentyl-9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-9H-purin-6-amine
0.00000046
3-(9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-6-[[4-(dimethylphosphoryl)phenyl]amino]-9H-purin-2-yl)propanenitrile
Homo sapiens
-
0.00004
3-([4-[(5-chloro-1,3-benzodioxol-4-yl)amino]pyrimidin-2-yl]amino)benzenesulfonamide
Mammalia
-
-
0.00055
3-([4-[(5-chloro-1,3-benzodioxol-4-yl)amino]pyrimidin-2-yl]amino)benzonitrile
Mammalia
-
-
0.0000097 - 0.00014
3-amino-5-((2R)-3-methylbutan-2-yl)-7-[5-(morpholin-4-yl)-pyridin-2-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.0000055 - 0.00007
3-amino-5-((2S)-3-methylbutan-2-yl)-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.00000055 - 0.000016
3-amino-5-((2S)-3-methylbutan-2-yl)-7-[1-methyl-5-(morpholin-4-yl)-1H-pyrazol-3-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.00000098 - 0.000024
3-amino-5-((2S)-3-methylbutan-2-yl)-7-[1-methyl-5-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-3-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]-pyridin-4-one
0.00000092 - 0.000007
3-amino-5-((2S)-3-methylbutan-2-yl)-7-[5-(morpholin-4-yl)-pyridin-2-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.000091 - 0.00083
3-amino-5-(2-methylpentan-3-yl)-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.0000063 - 0.00031
3-amino-5-(3-methylbutan-2-yl)-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.0000015 - 0.000015
3-amino-5-(3-methylbutan-2-yl)-7-[5-(morpholin-4-yl)pyridin-2-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.000012 - 0.00039
3-amino-5-isobutyl-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.000033 - 0.00018
3-amino-5-sec-butyl-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.0000012 - 0.000067
3-amino-7-[5-(1,1-dioxidothiomorpholin-4-yl)-1-methyl-1H-pyrazol-3-yl]-5-((2S)-3-methylbutan-2-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.0000021 - 0.000017
3-amino-7-[5-(2-hydroxypropan-2-yl)-1-methyl-1H-pyrazol-3-yl]-5-((2S)-3-methylbutan-2-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.000004
4-(2-fluoro-3-(4-oxoquinazolin-3(4H)-yl)phenyl)-7-(2-hydroxypropan-2-yl)-9H-carbazole-1-carboxamide
Mus musculus
at pH 7.4 and 22°C
0.000005
4-(2-methyl-3-(1-oxoisoindolin-2-yl)phenyl)-7-(4-methylpiperazine-1-carbonyl)-9H-carbazole-1-carboxamide
Mus musculus
at pH 7.4 and 22°C
0.000005
4-(3-(4-fluorobenzamido)-2-methylphenyl)-7-(4-methylpiperazine-1-carbonyl)-9H-carbazole-1-carboxamide
Mus musculus
at pH 7.4 and 22°C
0.000011
4-(3-(4-fluorobenzamido)-2-methylphenyl)-7-(isopropylamino)-9H-carbazole-1-carboxamide
Mus musculus
at pH 7.4 and 22°C
0.000005
4-(3-(5-fluoro-4-oxoquinazolin-3(4H)-yl)-2-methylphenyl)-7-(2-hydroxypropan-2-yl)-9H-carbazole-1-carboxamide
Mus musculus
at pH 7.4 and 22°C
0.000009
4-(3-(5-fluoropicolinamido)-2-methylphenyl)-7-(4-methylpiperazine-1-carbonyl)-9H-carbazole-1-carboxamide
Mus musculus
at pH 7.4 and 22°C
0.000002
4-(3-(6-fluoro-1-oxoisoindolin-2-yl)-2-methylphenyl)-7-(2-hydroxypropan-2-yl)-9H-carbazole-1-carboxamide
Mus musculus
at pH 7.4 and 22°C
0.000007
4-(3-(6-fluoro-4-oxoquinazolin-3(4H)-yl)-2-methylphenyl)-7-(2-hydroxypropan-2-yl)-9H-carbazole-1-carboxamide
Mus musculus
at pH 7.4 and 22°C
0.000002
4-(3-(7-fluoro-4-oxoquinazolin-3(4H)-yl)-2-methylphenyl)-7-(2-hydroxypropan-2-yl)-9H-carbazole-1-carboxamide
Mus musculus
at pH 7.4 and 22°C
0.000002
4-(3-(8-fluoro-4-oxoquinazolin-3(4H)-yl)-2-methylphenyl)-7-(2-hydroxypropan-2-yl)-9H-carbazole-1-carboxamide
Mus musculus
at pH 7.4 and 22°C
0.0003
4-([4-[(5-chloro-1,3-benzodioxol-4-yl)amino]pyrimidin-2-yl]amino)benzenesulfonamide
Mammalia
-
-
0.00125
4-([4-[(5-chloro-1,3-benzodioxol-4-yl)amino]pyrimidin-2-yl]amino)benzonitrile
Mammalia
-
-
0.000009
4-amino-5-(4-chlorophenyl)-7-(t-butyl)pyrazolo[3,4-d]pyrimidine
Mus musculus
-
substrate Csk binding protein, Cbp
0.0000008 - 0.000004
4-[4-([[3-tert-butyl-1-(quinolin-6-yl)-1H-pyrazol-5-yl]carbamoyl]amino)-3-fluorophenoxy]-N-methylpyridine-2-carboxamide
0.000003
7-(2-hydroxypropan-2-yl)-4-(2-methyl-3-(1-oxo-3,4-dihydroisoquinolin-2(1H)-yl)phenyl)-9H-carbazole-1-carboxamide
Mus musculus
at pH 7.4 and 22°C
0.000005
7-(2-hydroxypropan-2-yl)-4-(2-methyl-3-(1-oxoisoindolin-2-yl)phenyl)-9H-carbazole-1-carboxamide
Mus musculus
at pH 7.4 and 22°C
0.000005
7-(2-hydroxypropan-2-yl)-4-(2-methyl-3-(1-oxoisoquinolin-2(1H)-yl)phenyl)-9H-carbazole-1-carboxamide
Mus musculus
at pH 7.4 and 22°C
0.000044
7-(2-hydroxypropan-2-yl)-4-(3-(4-oxoquinazolin-3(4H)-yl)-phenyl)-9H-carbazole-1-carboxamide
Mus musculus
at pH 7.4 and 22°C
0.000003
7-(2-hydroxypropan-2-yl)-4-[2-methyl-3-(4-oxo-3,4-dihydroquinazolin-3-yl)phenyl]-9H-carbazole-1-carboxamide
Mus musculus
at pH 7.4 and 22°C
0.000003
7-(hydroxymethyl)-4-(2-methyl-3-(4-oxoquinazolin-3(4H)-yl)phenyl)-9H-carbazole-1-carboxamide
Mus musculus
at pH 7.4 and 22°C
0.00000046 - 0.00000732
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(1-methylethoxy)-9H-purin-6-amine
0.00000089 - 0.0000158
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(1-methylethyl)-9H-purin-6-amine
0.00000046
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(1-methylpiperidin-4-yl)-9H-purin-6-amine
Homo sapiens
-
0.00000046 - 0.00000163
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(1H-imidazol-1-yl)-9H-purin-6-amine
0.00000046 - 0.00000157
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(2-methoxyethoxy)-9H-purin-6-amine
0.00000023 - 0.0000068
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(4-methylpiperazin-1-yl)-9H-purin-6-amine
0.00000046 - 0.0000005
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(pyrrolidin-3-yloxy)-9H-purin-6-amine
0.00000046 - 0.0000018
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-methoxy-9H-purin-6-amine
0.00000023 - 0.00000302
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-morpholin-4-yl-9H-purin-6-amine
0.00000143 - 0.0000195
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-pyrrolidin-1-yl-9H-purin-6-amine
0.00000358 - 0.00000831
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-9H-purin-6-amine
0.00000178 - 0.00000593
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dipropylphosphoryl)phenyl]-2-(1-methylethyl)-9H-purin-6-amine
0.000004 - 0.0000173
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dipropylphosphoryl)phenyl]-9H-purin-6-amine
0.00000374 - 0.0000176
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N6-[4-(dimethylphosphoryl)phenyl]-N2,N2-dimethyl-9H-purine-2,6-diamine
0.00000277 - 0.00000556
9-[(E)-2-(2-chloro-6-methylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-9H-purin-6-amine
0.0000694 - 0.000126
9-[(E)-2-(2-chlorophenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-9H-purin-6-amine
0.00000658 - 0.0000543
9-[(Z)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dipropylphosphoryl)phenyl]-2-(1-methylethyl)-9H-purin-6-amine
0.000001
AP23464
Homo sapiens
-
0.0000008 - 0.000025
baricitinib
-
0.000037
BGB324
Homo sapiens
pH and temperature not specified in the publication
-
0.000005 - 0.000297
dasatinib
0.00036
epihematoxylol
Homo sapiens
-
0.0016
haematoxylene
Homo sapiens
-
0.0018
haematoxylone
Homo sapiens
-
0.00044
hematoxylin
Homo sapiens
-
0.00000065
ibrutinib
Homo sapiens
pH and temperature not specified in the publication
0.00000025 - 0.0000101
INCB16562
0.0000003 - 0.0000009
INCB20
-
0.0000172
LFM-A13
Mus musculus
-
-
0.00035
N-(5-chloro-1,3-benzodioxol-4-yl)-6-methoxy-7-(3-piperidin-1-ylpropoxy)quinazolin-4-amine
Mammalia
-
-
0.00296
N-(5-chloro-1,3-benzodioxol-4-yl)-N'-(3,4,5-trimethoxyphenyl)-1,3,5-triazine-2,4-diamine
Mammalia
-
-
0.00254
N-(5-chloro-1,3-benzodioxol-4-yl)-N'-(3,4,5-trimethoxyphenyl)pyrimidine-4,6-diamine
Mammalia
-
-
0.00016 - 0.0056
N-([[N2-(1-[4-[3-(4-[6-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]-2-methylpyrimidin-4-yl]piperazin-1-yl)-3-oxopropyl]-1H-1,2,3-triazol-1-yl]-28,32-dioxo-3,6,9,12,15,18,21,24,30-nonaoxa-27-azadotriacontan-32-yl)-L-glutaminyl]amino][4-(phosphonooxy)phenyl]acetyl)-L-alpha-glutamyl-alpha-glutamyl-L-isoleucinamide
0.00000236 - 0.000017
N-[4-(dimethylphosphoryl)phenyl]-9-[(E)-2-(1H-indazol-4-yl)ethenyl]-9H-purin-6-amine
0.0000167 - 0.000198
N-[4-(dimethylphosphoryl)phenyl]-9-[(E)-2-(1H-indol-4-yl)ethenyl]-9H-purin-6-amine
0.00000046
N-[4-(dimethylphosphoryl)phenyl]-9-[(E)-2-(5-methyl-1H-indazol-4-yl)ethenyl]-9H-purin-6-amine
Homo sapiens
-
0.0000318 - 0.0000733
N-[4-(dipropylphosphoryl)phenyl]-2-(1-methylethyl)-9-[(E)-2-phenylethenyl]-9H-purin-6-amine
0.000376 - 0.000626
N-[4-(dipropylphosphoryl)phenyl]-2-(1-methylethyl)-9-[(Z)-2-phenylethenyl]-9H-purin-6-amine
0.01132
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(2-chlorophenyl)pyrimidine-2,4-diamine
Mammalia
-
-
0.005
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(2-fluorophenyl)pyrimidine-2,4-diamine
Mammalia
-
-
0.00388
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(2-methoxyphenyl)pyrimidine-2,4-diamine
Mammalia
-
-
0.01396
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(2-methylphenyl)pyrimidine-2,4-diamine
Mammalia
-
-
0.00785
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(2-morpholin-4-ylphenyl)pyrimidine-2,4-diamine
Mammalia
-
-
0.00024
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(3,4,5-trimethoxyphenyl)pyrimidine-2,4-diamine
Mammalia
-
-
0.00133
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(3-chlorophenyl)pyrimidine-2,4-diamine
Mammalia
-
-
0.00115
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(3-fluorophenyl)pyrimidine-2,4-diamine
Mammalia
-
-
0.00064
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(3-methoxyphenyl)pyrimidine-2,4-diamine
Mammalia
-
-
0.00046
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(3-methylphenyl)pyrimidine-2,4-diamine
Mammalia
-
-
0.00058
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(3-morpholin-4-ylphenyl)pyrimidine-2,4-diamine
Mammalia
-
-
0.006
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(4-chlorophenyl)pyrimidine-2,4-diamine
Mammalia
-
-
0.0023
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(4-fluorophenyl)pyrimidine-2,4-diamine
Mammalia
-
-
0.00194
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(4-methoxyphenyl)pyrimidine-2,4-diamine
Mammalia
-
-
0.0016
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(4-methylphenyl)pyrimidine-2,4-diamine
Mammalia
-
-
0.001
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(4-morpholin-4-ylphenyl)pyrimidine-2,4-diamine
Mammalia
-
-
0.00155
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-phenylpyrimidine-2,4-diamine
Mammalia
-
-
0.041
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-[2-(methylsulfonyl)phenyl]pyrimidine-2,4-diamine
Mammalia
-
-
0.00009
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-[3-(methylsulfonyl)phenyl]pyrimidine-2,4-diamine
Mammalia
-
-
0.00063
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-[4-(methylsulfonyl)phenyl]pyrimidine-2,4-diamine
Mammalia
-
-
0.000025
nilotinib
Homo sapiens
-
ABL1
0.00001
ON012380
Homo sapiens
-
below, inhibition of BCR-ABL
0.000001
SKI-606
Homo sapiens
-
inhibition of BCR-ABL
0.008
staurosporine
Homo sapiens
-
i.e. ST, inhibition of Syk and Lyn, IC50 for Syk is 0.008 mM
0.000035
SU6656
Mus musculus
-
substrate Csk binding protein, Cbp
additional information
additional information
-
0.0029
1-(4-[6-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]-2-methylpyrimidin-4-yl]piperazin-1-yl)-3-(1-nonadecyl-1H-1,2,3-triazol-4-yl)propan-1-one
Homo sapiens
3-domain c-Src kinase, pH and temperature not specified in the publication
0.0046
1-(4-[6-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]-2-methylpyrimidin-4-yl]piperazin-1-yl)-3-(1-nonadecyl-1H-1,2,3-triazol-4-yl)propan-1-one
Homo sapiens
pH and temperature not specified in the publication
0.0089
1-(4-[6-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]-2-methylpyrimidin-4-yl]piperazin-1-yl)-3-(1-nonadecyl-1H-1,2,3-triazol-4-yl)propan-1-one
Homo sapiens
pH and temperature not specified in the publication
0.0093
1-(4-[6-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]-2-methylpyrimidin-4-yl]piperazin-1-yl)-3-(1-nonadecyl-1H-1,2,3-triazol-4-yl)propan-1-one
Homo sapiens
pH and temperature not specified in the publication
0.0096
1-(4-[6-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]-2-methylpyrimidin-4-yl]piperazin-1-yl)-3-(1-nonadecyl-1H-1,2,3-triazol-4-yl)propan-1-one
Homo sapiens
pH and temperature not specified in the publication
0.0108
1-(4-[6-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]-2-methylpyrimidin-4-yl]piperazin-1-yl)-3-(1-nonadecyl-1H-1,2,3-triazol-4-yl)propan-1-one
Homo sapiens
pH and temperature not specified in the publication
0.0218
1-(4-[6-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]-2-methylpyrimidin-4-yl]piperazin-1-yl)-3-(1-nonadecyl-1H-1,2,3-triazol-4-yl)propan-1-one
Homo sapiens
pH and temperature not specified in the publication
0.00000129
2-cyclopentyl-9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-9H-purin-6-amine
Homo sapiens
-
0.0000323
2-cyclopentyl-9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-9H-purin-6-amine
Homo sapiens
-
0.0000097
3-amino-5-((2R)-3-methylbutan-2-yl)-7-[5-(morpholin-4-yl)-pyridin-2-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.000085
3-amino-5-((2R)-3-methylbutan-2-yl)-7-[5-(morpholin-4-yl)-pyridin-2-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.0001
3-amino-5-((2R)-3-methylbutan-2-yl)-7-[5-(morpholin-4-yl)-pyridin-2-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.00014
3-amino-5-((2R)-3-methylbutan-2-yl)-7-[5-(morpholin-4-yl)-pyridin-2-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.0000055
3-amino-5-((2S)-3-methylbutan-2-yl)-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.0000064
3-amino-5-((2S)-3-methylbutan-2-yl)-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.00003
3-amino-5-((2S)-3-methylbutan-2-yl)-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.00007
3-amino-5-((2S)-3-methylbutan-2-yl)-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.00000055
3-amino-5-((2S)-3-methylbutan-2-yl)-7-[1-methyl-5-(morpholin-4-yl)-1H-pyrazol-3-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.0000028
3-amino-5-((2S)-3-methylbutan-2-yl)-7-[1-methyl-5-(morpholin-4-yl)-1H-pyrazol-3-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.000014
3-amino-5-((2S)-3-methylbutan-2-yl)-7-[1-methyl-5-(morpholin-4-yl)-1H-pyrazol-3-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.000016
3-amino-5-((2S)-3-methylbutan-2-yl)-7-[1-methyl-5-(morpholin-4-yl)-1H-pyrazol-3-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.00000098
3-amino-5-((2S)-3-methylbutan-2-yl)-7-[1-methyl-5-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-3-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]-pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.0000046
3-amino-5-((2S)-3-methylbutan-2-yl)-7-[1-methyl-5-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-3-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]-pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.000012
3-amino-5-((2S)-3-methylbutan-2-yl)-7-[1-methyl-5-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-3-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]-pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.000024
3-amino-5-((2S)-3-methylbutan-2-yl)-7-[1-methyl-5-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-3-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]-pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.00000092
3-amino-5-((2S)-3-methylbutan-2-yl)-7-[5-(morpholin-4-yl)-pyridin-2-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.0000023
3-amino-5-((2S)-3-methylbutan-2-yl)-7-[5-(morpholin-4-yl)-pyridin-2-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.0000069
3-amino-5-((2S)-3-methylbutan-2-yl)-7-[5-(morpholin-4-yl)-pyridin-2-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.000007
3-amino-5-((2S)-3-methylbutan-2-yl)-7-[5-(morpholin-4-yl)-pyridin-2-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.000091
3-amino-5-(2-methylpentan-3-yl)-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.000092
3-amino-5-(2-methylpentan-3-yl)-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.00026
3-amino-5-(2-methylpentan-3-yl)-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.00083
3-amino-5-(2-methylpentan-3-yl)-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.0000063
3-amino-5-(3-methylbutan-2-yl)-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.000032
3-amino-5-(3-methylbutan-2-yl)-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.000079
3-amino-5-(3-methylbutan-2-yl)-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.00031
3-amino-5-(3-methylbutan-2-yl)-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.0000015
3-amino-5-(3-methylbutan-2-yl)-7-[5-(morpholin-4-yl)pyridin-2-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.0000053
3-amino-5-(3-methylbutan-2-yl)-7-[5-(morpholin-4-yl)pyridin-2-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.000013
3-amino-5-(3-methylbutan-2-yl)-7-[5-(morpholin-4-yl)pyridin-2-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.000015
3-amino-5-(3-methylbutan-2-yl)-7-[5-(morpholin-4-yl)pyridin-2-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.000012
3-amino-5-isobutyl-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.000072
3-amino-5-isobutyl-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.00023
3-amino-5-isobutyl-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.00039
3-amino-5-isobutyl-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.000033
3-amino-5-sec-butyl-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.000052
3-amino-5-sec-butyl-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.000091
3-amino-5-sec-butyl-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.00018
3-amino-5-sec-butyl-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.0000012
3-amino-7-[5-(1,1-dioxidothiomorpholin-4-yl)-1-methyl-1H-pyrazol-3-yl]-5-((2S)-3-methylbutan-2-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.0000046
3-amino-7-[5-(1,1-dioxidothiomorpholin-4-yl)-1-methyl-1H-pyrazol-3-yl]-5-((2S)-3-methylbutan-2-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.000013
3-amino-7-[5-(1,1-dioxidothiomorpholin-4-yl)-1-methyl-1H-pyrazol-3-yl]-5-((2S)-3-methylbutan-2-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.000067
3-amino-7-[5-(1,1-dioxidothiomorpholin-4-yl)-1-methyl-1H-pyrazol-3-yl]-5-((2S)-3-methylbutan-2-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.0000021
3-amino-7-[5-(2-hydroxypropan-2-yl)-1-methyl-1H-pyrazol-3-yl]-5-((2S)-3-methylbutan-2-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.0000033
3-amino-7-[5-(2-hydroxypropan-2-yl)-1-methyl-1H-pyrazol-3-yl]-5-((2S)-3-methylbutan-2-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.000016
3-amino-7-[5-(2-hydroxypropan-2-yl)-1-methyl-1H-pyrazol-3-yl]-5-((2S)-3-methylbutan-2-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.000017
3-amino-7-[5-(2-hydroxypropan-2-yl)-1-methyl-1H-pyrazol-3-yl]-5-((2S)-3-methylbutan-2-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.0000008
4-[4-([[3-tert-butyl-1-(quinolin-6-yl)-1H-pyrazol-5-yl]carbamoyl]amino)-3-fluorophenoxy]-N-methylpyridine-2-carboxamide
Homo sapiens
wild-type, pH not specified in the publication, temperature not specified in the publication
0.000004
4-[4-([[3-tert-butyl-1-(quinolin-6-yl)-1H-pyrazol-5-yl]carbamoyl]amino)-3-fluorophenoxy]-N-methylpyridine-2-carboxamide
Homo sapiens
mutant T315I, pH not specified in the publication, temperature not specified in the publication
0.00000046
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(1-methylethoxy)-9H-purin-6-amine
Homo sapiens
-
0.00000732
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(1-methylethoxy)-9H-purin-6-amine
Homo sapiens
-
0.00000089
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(1-methylethyl)-9H-purin-6-amine
Homo sapiens
-
0.0000158
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(1-methylethyl)-9H-purin-6-amine
Homo sapiens
-
0.00000046
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(1H-imidazol-1-yl)-9H-purin-6-amine
Homo sapiens
-
0.00000163
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(1H-imidazol-1-yl)-9H-purin-6-amine
Homo sapiens
-
0.00000046
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(2-methoxyethoxy)-9H-purin-6-amine
Homo sapiens
-
0.00000157
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(2-methoxyethoxy)-9H-purin-6-amine
Homo sapiens
-
0.00000023
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(4-methylpiperazin-1-yl)-9H-purin-6-amine
Homo sapiens
-
0.0000068
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(4-methylpiperazin-1-yl)-9H-purin-6-amine
Homo sapiens
-
0.00000046
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(pyrrolidin-3-yloxy)-9H-purin-6-amine
Homo sapiens
-
0.0000005
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(pyrrolidin-3-yloxy)-9H-purin-6-amine
Homo sapiens
-
0.00000046
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-methoxy-9H-purin-6-amine
Homo sapiens
-
0.0000018
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-methoxy-9H-purin-6-amine
Homo sapiens
-
0.00000023
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-morpholin-4-yl-9H-purin-6-amine
Homo sapiens
-
0.00000302
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-morpholin-4-yl-9H-purin-6-amine
Homo sapiens
-
0.00000143
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-pyrrolidin-1-yl-9H-purin-6-amine
Homo sapiens
-
0.0000195
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-pyrrolidin-1-yl-9H-purin-6-amine
Homo sapiens
-
0.00000358
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-9H-purin-6-amine
Homo sapiens
-
0.00000831
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-9H-purin-6-amine
Homo sapiens
-
0.00000178
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dipropylphosphoryl)phenyl]-2-(1-methylethyl)-9H-purin-6-amine
Homo sapiens
-
0.00000593
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dipropylphosphoryl)phenyl]-2-(1-methylethyl)-9H-purin-6-amine
Homo sapiens
-
0.000004
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dipropylphosphoryl)phenyl]-9H-purin-6-amine
Homo sapiens
-
0.0000173
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dipropylphosphoryl)phenyl]-9H-purin-6-amine
Homo sapiens
-
0.00000374
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N6-[4-(dimethylphosphoryl)phenyl]-N2,N2-dimethyl-9H-purine-2,6-diamine
Homo sapiens
-
0.0000176
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N6-[4-(dimethylphosphoryl)phenyl]-N2,N2-dimethyl-9H-purine-2,6-diamine
Homo sapiens
-
0.00000277
9-[(E)-2-(2-chloro-6-methylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-9H-purin-6-amine
Homo sapiens
-
0.00000556
9-[(E)-2-(2-chloro-6-methylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-9H-purin-6-amine
Homo sapiens
-
0.0000694
9-[(E)-2-(2-chlorophenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-9H-purin-6-amine
Homo sapiens
-
0.000126
9-[(E)-2-(2-chlorophenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-9H-purin-6-amine
Homo sapiens
-
0.00000658
9-[(Z)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dipropylphosphoryl)phenyl]-2-(1-methylethyl)-9H-purin-6-amine
Homo sapiens
-
0.0000543
9-[(Z)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dipropylphosphoryl)phenyl]-2-(1-methylethyl)-9H-purin-6-amine
Homo sapiens
-
0.0102
AG490
Homo sapiens
-
JAK1, in 50 mM, Tris-HCl (pH 7.8), 100 mM NaCl, 5 mM dithiothreitol, and 0.1 mg/ml bovine serum albumin, at 25°C
0.0112
AG490
Homo sapiens
-
JAK2, in 50 mM, Tris-HCl (pH 7.8), 100 mM NaCl, 5 mM dithiothreitol, and 0.1 mg/ml bovine serum albumin, at 25°C
0.0154
AG490
Homo sapiens
-
JAK3, in 50 mM, Tris-HCl (pH 7.8), 100 mM NaCl, 5 mM dithiothreitol, and 0.1 mg/ml bovine serum albumin, at 25°C
0.0000008
baricitinib
Homo sapiens
37°C, pH not specified in the publication
-
0.00000099
baricitinib
Homo sapiens
37°C, pH not specified in the publication
-
0.0000087
baricitinib
Homo sapiens
37°C, pH not specified in the publication
-
0.000025
baricitinib
Homo sapiens
37°C, pH not specified in the publication
-
0.000005
dasatinib
Homo sapiens
-
inhibition of Btk kinase, pH 7.5
0.000011
dasatinib
Mus musculus
-
substrate Csk binding protein, Cbp
0.000014
dasatinib
Homo sapiens
-
inhibition of Abl kinase, pH 7.5
0.000228
dasatinib
Homo sapiens
-
inhibition of Itk F435T kinase mutant, pH 7.5
0.000297
dasatinib
Homo sapiens
-
inhibition of Tec kinase, pH 7.5
0.00000025
INCB16562
Homo sapiens
-
JAK2
0.0000022
INCB16562
Homo sapiens
-
JAK1
0.0000027
INCB16562
Homo sapiens
-
TYK2
0.0000101
INCB16562
Homo sapiens
-
JAK3
0.0000003
INCB20
Homo sapiens
-
TYK2, in 50 mM, Tris-HCl (pH 7.8), 100 mM NaCl, 5 mM dithiothreitol, and 0.1 mg/ml bovine serum albumin, at 25°C
-
0.0000005
INCB20
Homo sapiens
-
JAK2, in 50 mM, Tris-HCl (pH 7.8), 100 mM NaCl, 5 mM dithiothreitol, and 0.1 mg/ml bovine serum albumin, at 25°C
-
0.0000005
INCB20
Homo sapiens
-
JAK3, in 50 mM, Tris-HCl (pH 7.8), 100 mM NaCl, 5 mM dithiothreitol, and 0.1 mg/ml bovine serum albumin, at 25°C
-
0.0000009
INCB20
Homo sapiens
-
JAK1, in 50 mM, Tris-HCl (pH 7.8), 100 mM NaCl, 5 mM dithiothreitol, and 0.1 mg/ml bovine serum albumin, at 25°C
-
0.00093
LS104
Homo sapiens
in the presence of 0.02 mM ATP and 0.00015 mM substrate peptide
0.00193
LS104
Homo sapiens
in the presence of 0.02 mM ATP and 0.0003 mM substrate peptide
0.00252
LS104
Homo sapiens
in the presence of 0.02 mM ATP and 0.0015 mM substrate peptide
0.00016
N-([[N2-(1-[4-[3-(4-[6-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]-2-methylpyrimidin-4-yl]piperazin-1-yl)-3-oxopropyl]-1H-1,2,3-triazol-1-yl]-28,32-dioxo-3,6,9,12,15,18,21,24,30-nonaoxa-27-azadotriacontan-32-yl)-L-glutaminyl]amino][4-(phosphonooxy)phenyl]acetyl)-L-alpha-glutamyl-alpha-glutamyl-L-isoleucinamide
Homo sapiens
3-domain c-Src kinase, pH and temperature not specified in the publication
0.0025
N-([[N2-(1-[4-[3-(4-[6-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]-2-methylpyrimidin-4-yl]piperazin-1-yl)-3-oxopropyl]-1H-1,2,3-triazol-1-yl]-28,32-dioxo-3,6,9,12,15,18,21,24,30-nonaoxa-27-azadotriacontan-32-yl)-L-glutaminyl]amino][4-(phosphonooxy)phenyl]acetyl)-L-alpha-glutamyl-alpha-glutamyl-L-isoleucinamide
Homo sapiens
pH and temperature not specified in the publication
0.0028
N-([[N2-(1-[4-[3-(4-[6-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]-2-methylpyrimidin-4-yl]piperazin-1-yl)-3-oxopropyl]-1H-1,2,3-triazol-1-yl]-28,32-dioxo-3,6,9,12,15,18,21,24,30-nonaoxa-27-azadotriacontan-32-yl)-L-glutaminyl]amino][4-(phosphonooxy)phenyl]acetyl)-L-alpha-glutamyl-alpha-glutamyl-L-isoleucinamide
Homo sapiens
pH and temperature not specified in the publication
0.0031
N-([[N2-(1-[4-[3-(4-[6-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]-2-methylpyrimidin-4-yl]piperazin-1-yl)-3-oxopropyl]-1H-1,2,3-triazol-1-yl]-28,32-dioxo-3,6,9,12,15,18,21,24,30-nonaoxa-27-azadotriacontan-32-yl)-L-glutaminyl]amino][4-(phosphonooxy)phenyl]acetyl)-L-alpha-glutamyl-alpha-glutamyl-L-isoleucinamide
Homo sapiens
pH and temperature not specified in the publication
0.0053
N-([[N2-(1-[4-[3-(4-[6-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]-2-methylpyrimidin-4-yl]piperazin-1-yl)-3-oxopropyl]-1H-1,2,3-triazol-1-yl]-28,32-dioxo-3,6,9,12,15,18,21,24,30-nonaoxa-27-azadotriacontan-32-yl)-L-glutaminyl]amino][4-(phosphonooxy)phenyl]acetyl)-L-alpha-glutamyl-alpha-glutamyl-L-isoleucinamide
Homo sapiens
pH and temperature not specified in the publication
0.0056
N-([[N2-(1-[4-[3-(4-[6-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]-2-methylpyrimidin-4-yl]piperazin-1-yl)-3-oxopropyl]-1H-1,2,3-triazol-1-yl]-28,32-dioxo-3,6,9,12,15,18,21,24,30-nonaoxa-27-azadotriacontan-32-yl)-L-glutaminyl]amino][4-(phosphonooxy)phenyl]acetyl)-L-alpha-glutamyl-alpha-glutamyl-L-isoleucinamide
Homo sapiens
pH and temperature not specified in the publication
0.00000236
N-[4-(dimethylphosphoryl)phenyl]-9-[(E)-2-(1H-indazol-4-yl)ethenyl]-9H-purin-6-amine
Homo sapiens
-
0.000017
N-[4-(dimethylphosphoryl)phenyl]-9-[(E)-2-(1H-indazol-4-yl)ethenyl]-9H-purin-6-amine
Homo sapiens
-
0.0000167
N-[4-(dimethylphosphoryl)phenyl]-9-[(E)-2-(1H-indol-4-yl)ethenyl]-9H-purin-6-amine
Homo sapiens
-
0.000198
N-[4-(dimethylphosphoryl)phenyl]-9-[(E)-2-(1H-indol-4-yl)ethenyl]-9H-purin-6-amine
Homo sapiens
-
0.0000318
N-[4-(dipropylphosphoryl)phenyl]-2-(1-methylethyl)-9-[(E)-2-phenylethenyl]-9H-purin-6-amine
Homo sapiens
-
0.0000733
N-[4-(dipropylphosphoryl)phenyl]-2-(1-methylethyl)-9-[(E)-2-phenylethenyl]-9H-purin-6-amine
Homo sapiens
-
0.000376
N-[4-(dipropylphosphoryl)phenyl]-2-(1-methylethyl)-9-[(Z)-2-phenylethenyl]-9H-purin-6-amine
Homo sapiens
-
0.000626
N-[4-(dipropylphosphoryl)phenyl]-2-(1-methylethyl)-9-[(Z)-2-phenylethenyl]-9H-purin-6-amine
Homo sapiens
-
additional information
additional information
Mus musculus
-
-
-
additional information
additional information
Homo sapiens
-
-
-
additional information
additional information
Rattus norvegicus
-
-
-
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N114A
Abelson leukaemia virus
-
site-directed mutagenesis in the proline-rich region, mutant of the SH3 domain, structure determination in a complex with a proline-rich peptide, comparison to the wild-type enzyme, overview
K711E
substitution in the catalytic domain of RLK5 results in the catalytically inactive protein
E695K
-
mutation in the JH2 domain of the Jak homologue hopscotch, which renders the kinase hyperactive and causes hematopoietic hyperplasia
R614A
mutant, used in autokinase activity assay
R614K
mutant, used in autokinase activity assay
Y574A
mutant, used in autokinase activity assay
Y574E
mutant, used in autokinase activity assay
Y574F
mutant, used in autokinase activity assay
Y574G
mutant, used in autokinase activity assay
Y574N
mutant, used in autokinase activity assay
E1025D
the mutation causes a complete ts phenotype
H559R
mutation results in a partial temperature sensitivity
A356N
the mutation increases enzyme activity
A433T
naturally occuring mutation in kinase ABL1 of chronic myeloid leukemia patients
C616Y
-
the JAK2 mutation is associated with polycythemia vera
C618R
-
the JAK2 mutation is associated with polycythemia vera
D276A
-
site-directed mutagenesis, reduced activity with substrates poly(Glu4-Tyr) and [kdSrc kinase]-L-tyrosine compared to the wild-type enzyme
D276G
naturally occuring mutation in kinase ABL1 of chronic myeloid leukemia patients
D332A
-
site-directed mutagenesis of Csk in the DFG motif in front of the activation loop leads to complete loss of kinase activity
D344A
-
site-directed mutagenesis of Csk in the activation loop, mutant shows slightly increased activity with kdSrc and slightly reduced activity with poly(Glu4-Tyr) as substrates compared to the wild-type enzyme
D382N
-
site-directed mutagenesis, catalytically inactive mutant
D518A
-
site-directed mutagenesis of Src, the mutant enzyme shows reduced interaction with the Csk and reduced inactivation by Csk
D518E
-
site-directed mutagenesis of Src, the mutant enzyme shows reduced interaction with the Csk and reduced inactivation by Csk
D518G
-
site-directed mutagenesis of Src, the mutant enzyme shows reduced interaction with the Csk and reduced inactivation by Csk
D518N
-
site-directed mutagenesis of Src, the mutant enzyme shows reduced interaction with the Csk and reduced inactivation by Csk
D620E
-
the JAK2 mutation is associated with myeloproliferative syndrome and polycythemia vera
D639Y
missense mutation in the SH1 domain, cG2078->T
dN541-R544
deletion in the SH1 domain, cG1513-G1794
dW281-G325
deletion in the SH2 domain, cG1003-G1137
E225K
-
naturally occurring mutation in the BCR/ABL kinase leading to resistance against inhibitor imatinib mesylate in vivo and in cell culture in vitro
E225V
-
naturally occurring mutation in the BCR/ABL kinase leading to resistance against inhibitor imatinib mesylate in cell culture in vitro
E300A
-
site-directed mutagenesis, reduced activity with substrates poly(Glu4-Tyr) and [kdSrc kinase]-L-tyrosine compared to the wild-type enzyme
E324A
-
site-directed mutagenesis of Csk, the mutant enzyme shows unaltered interaction with the Src substrate, and slightly reduced activity with the polyEY substrate
E338A
-
site-directed mutagenesis of Csk in the activation loop, mutant shows 40-60% remaining activity compared to the wild-type enzyme
E355A
naturally occuring mutation in kinase ABL1 of chronic myeloid leukemia patients
E355G
naturally occuring mutation in kinase ABL1 of chronic myeloid leukemia patients
E453K
naturally occuring mutation in kinase ABL1 of chronic myeloid leukemia patients
E459G
naturally occuring mutation in kinase ABL1 of chronic myeloid leukemia patients
E459K
naturally occuring mutation in kinase ABL1 of chronic myeloid leukemia patients
E459Q
naturally occuring mutation in kinase ABL1 of chronic myeloid leukemia patients
E510A
-
site-directed mutagenesis of Src, the mutant enzyme shows reduced interaction with the Csk and reduced inactivation by Csk
E510R
-
site-directed mutagenesis of Src, the mutant enzyme shows reduced interaction with the Csk and reduced inactivation by Csk
E605G
missense mutation in the SH1 domain, cA1977->G
E627E
-
the JAK2 mutation is associated with myeloproliferative disorder
E864K
-
mutation is sufficient to support growth and downstream signaling at high concentrations of 2-(1,1-dimethylethyl)-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinolin-7-one, i.e. JAK inhibitor-I
F183A
-
site-directed mutagenesis, about 70% reduced Csk tyrosine kinase activity compared to the wild-type enzyme
F183L
-
site-directed mutagenesis, about 40% reduced Csk tyrosine kinase activity compared to the wild-type enzyme
F183W
-
site-directed mutagenesis, about 50% reduced Csk tyrosine kinase activity compared to the wild-type enzyme
F311I
naturally occuring mutation in kinase ABL1 of chronic myeloid leukemia patients
F317L
naturally occuring mutation in kinase ABL1 of chronic myeloid leukemia patients
F359C
naturally occuring mutation in kinase ABL1 of chronic myeloid leukemia patients
F359V
naturally occuring mutation in kinase ABL1 of chronic myeloid leukemia patients
F382A
-
site-directed mutagenesis, reduced activity with substrate poly(Glu4-Tyr), and highly redcuced activity with substrate [kdSrc kinase]-L-tyrosine compared to the wild-type enzyme
F486S
naturally occuring mutation in kinase ABL1 of chronic myeloid leukemia patients
F540S
mutant, shows absence of Btk phosphorylation on Tyr223
FSdG299X321
deletion in the SH2 domain, cG1058-G1137
FSdN450X457
deletion in the SH1 domain, cG1513-G1729
FSiF583X597
insertion in the SH1 domain, 518 bp insertion between exon 17 and exon 18
FSiG299X312
insertion in the SH2 domain, 579 bp insertion between exon 10 and exon 11
G250E
naturally occuring mutation in kinase ABL1 of chronic myeloid leukemia patients
G2A/C3A
mutant lacking the sites for lipid modification
G2A/C3A/K275A
mutant lacking the sites for lipid modification, mutation in the ATP-binding site, kinase-dead
G346A
-
site-directed mutagenesis of Csk in the activation loop, mutant shows decreased activity compared to the wild-type enzyme
G831R
-
mutation is sufficient to support growth and downstream signaling at high concentrations of 2-(1,1-dimethylethyl)-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinolin-7-one, i.e. JAK inhibitor-I
G935R
-
mutation is sufficient to support growth and downstream signaling at high concentrations of 2-(1,1-dimethylethyl)-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinolin-7-one, i.e. JAK inhibitor-I. Mutant retains kinase activity exceeding 130 microM JAK inhibitor-I
H384A
-
site-directed mutagenesis, the mutant shows reduced activity compared to the wild-type Src
H384Q
-
site-directed mutagenesis, the mutant shows reduced activity compared to the wild-type Src
H384Q/Y416F
-
site-directed mutagenesis, the mutant shows reduced activity compared to the wild-type Src
H384Y
-
site-directed mutagenesis, the mutant shows reduced activity and no autophosphorylation compared to the wild-type Src
H384Y/Y416F
-
site-directed mutagenesis, the mutant shows reduced activity compared to the wild-type Src
H384Y/Y527F
-
site-directed mutagenesis, the mutant shows reduced activity compared to the wild-type Src
H396R
naturally occuring mutation in kinase ABL1 of chronic myeloid leukemia patients
IFiM450+27
insertion in the SH2 domain, 81 bp insertion between exon 14 and exon 15
K222R
-
site-directed mutagenesis, about 80% reduced Csk tyrosine kinase activity compared to the wild-type enzyme
K247L
naturally occuring mutation in kinase ABL1 of chronic myeloid leukemia patients
K267M
-
a Hck mutant, the inability of HckK267M to undergo autophosphorylation promotes its phosphorylation at YT by CSK to a higher extent than that of wild type Hck
K274M
-
Lyn mutant, Lyn K274M does not form a stable protein complex with CHK, whereas its unphosphorylated counterpart does
K290M
-
a kinase-inactive Abl mutant
K298M
-
site-directed mutagenesis, a dominant-negative enzyme mutant
K299M
-
inactive mutant, interacts with TCGAP, coexpression of FynY531F, SH2-defective R176K, and SH3-defective P134K mutants, but not K299M, with TCGAP enhance tyrosine phosphorylation of TCGAP
K337A
-
site-directed mutagenesis of Csk in the activation loop, mutant shows slightly decreased activity compared to the wild-type enzyme
K361G/K362A
-
the mutant shows reduced phosphorylation activity compared to the wild-type enzyme, especially with substrate poly(Glu4-Tyr)
K374N
mutant, residual kinase activity is present
K430E
mutant, shows absence of Btk phosphorylation on Tyr223
K457A
-
site-directed mutagenesis, mutation leads to increase in phosphorylation sites on the substrate FGFR3
K539L
-
the JAK2 mutation is associated with polycythemia vera
K590E
-
site-directed mutagenesis, inactive mutant enzyme
K607N
-
the JAK2 mutation is associated with acute myelogenous leukemia
K882E
-
kinase-inactive JAK2 mutant
L111P
missense mutation in the PH domain, cT497->C
L111P/R288W/R544S/R562W/S578P/E605G/D639Y/R641H
mutations are due to deletions and insertions of exons and introns, respectively, which suggest splicing defects, leading to development of the X-linked agammaglobulinemia, XLA, a humoral primary immunodeficiency, in which affected patients have very low levels of peripheral B cells and a profound deficiency of all immunoglobulin isotypes, overview
L145P/L334P
-
site-directed mutagenesis, mutation in the first and second coiled-coil motifs, mutations lead to growth arrest of yeast cells
L145P/R483L
-
mutant enzyme shows low c-Fes colocalization with microtubules
L223A
-
site-directed mutagenesis, about 40% reduced Csk tyrosine kinase activity compared to the wild-type enzyme
L223F
-
site-directed mutagenesis, only slightly reduced Csk tyrosine kinase activity compared to the wild-type enzyme
L248V
naturally occuring mutation in kinase ABL1 of chronic myeloid leukemia patients
L296A
-
site-directed mutagenesis of Csk, the mutant enzyme shows reduced interaction with the Src substrate, and reduced activity with the polyEY substrate
L298V
naturally occuring mutation in kinase ABL1 of chronic myeloid leukemia patients
L334P
-
site-directed mutagenesis, mutation in the second coiled-coil motif, mutation leads to growth arrest of yeast cells
L364I
naturally occuring mutation in kinase ABL1 of chronic myeloid leukemia patients
L611S
-
the JAK2 mutation is associated with acute lymphocytic leukemia
M244V
naturally occuring mutation in kinase ABL1 of chronic myeloid leukemia patients
M351I
-
naturally occuring Abl mutant, the mutant is inhibitor imatinib-resistant
M351T
naturally occuring mutation in kinase ABL1 of chronic myeloid leukemia patients
M929I
-
mutation is sufficient to support growth and downstream signaling at high concentrations of 2-(1,1-dimethylethyl)-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinolin-7-one, i.e. JAK inhibitor-I
N326A
-
site-directed mutagenesis of Csk, the mutant enzyme shows reduced interaction with the Src substrate, and reduced activity with the polyEY substrate
N391D
-
site-directed mutagenesis, the mutant shows highly reduced enzyme activity and can be well expressed and purified using the Escherichia coli expression system
N909K
-
mutation is sufficient to support growth and downstream signaling at high concentrations of 2-(1,1-dimethylethyl)-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinolin-7-one, i.e. JAK inhibitor-I
P1057S
-
mutation is sufficient to support growth and downstream signaling at high concentrations of 2-(1,1-dimethylethyl)-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinolin-7-one, i.e. JAK inhibitor-I
P131L
-
a SH3-domain mutant with increased activity compared to wild-type Abl
P134L
-
an SH3-defective mutant, no interaction with TCGAP, coexpression of FynY531F, SH2-defective R176K, and SH3-defective P134K mutants, but not K299M, with TCGAP enhance tyrosine phosphorylation of TCGAP
Pyk2K457A
-
Pyk2MT, dominant negative Pyk2 mutant, inactive
Q343A
-
site-directed mutagenesis of Csk in the activation loop, mutant shows slightly decreased activity compared to the wild-type enzyme
R1127K
-
mutation is sufficient to support growth and downstream signaling at high concentrations of 2-(1,1-dimethylethyl)-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinolin-7-one, i.e. JAK inhibitor-I
R171K
-
SH2 domain variant containing a mutation
R176K
-
an SH2-defective mutant, interacts with TCGAP, coexpression of FynY531F, SH2-defective R176K, and SH3-defective P134K mutants, but not K299M, with TCGAP enhance tyrosine phosphorylation of TCGAP
R279A
-
site-directed mutagenesis of Csk, the mutant enzyme shows reduced interaction with the Src substrate
R281A
-
site-directed mutagenesis of Csk, the mutant enzyme shows reduced interaction with the Src substrate
R281A/R283A
-
site-directed mutagenesis, about 90% reduced activity with substrate [kdSrc kinase]-L-tyrosine compared to the wild-type enzyme
R283E
-
site-directed mutagenesis of Csk, the mutant enzyme shows highly reduced interaction with the Src substrate
R283K
-
site-directed mutagenesis of Csk, the mutant enzyme shows highly reduced interaction with the Src substrate
R313A
-
site-directed mutagenesis, activity similar to the wild-type enzyme
R388A/A390R
-
site-directed mutagenesis, mutations in the catalytic loop, the mutant shows slightly reduced enzyme activity and cannot be well expressed and purified using the Escherichia coli expression system
R389A
-
the mutant shows reduced phosphorylation activity compared to the wild-type enzyme, especially with substrate [kdSrc kinase]-L-tyrosine
R483L
-
mutation reverses the c-Fes colocalization with microtubules
R544G
mutant, residual kinase activity is present
R562W
missense mutation in the SH1 domain, cC1847->T
R641H
missense mutation in the SH1 domain, cG2085->A
R975G
-
mutation is sufficient to support growth and downstream signaling at high oncentrations of 2-(1,1-dimethylethyl)-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinolin-7-one, i.e. JAK inhibitor-I
S273A
-
site-directed mutagenesis, reduced activity with substrate [kdSrc kinase]-L-tyrosine compared to the wild-type enzyme
S280A/R281A/R283A/F381A
-
site-directed mutagenesis, about 90% reduced activity with substrate [kdSrc kinase]-L-tyrosine compared to the wild-type enzyme
S284A
-
site-directed mutagenesis, reduced activity with substrates poly(Glu4-Tyr) and [kdSrc kinase]-L-tyrosine compared to the wild-type enzyme
S340A
-
site-directed mutagenesis of Csk in the activation loop, mutant shows slightly decreased activity compared to the wild-type enzyme
S341A
-
site-directed mutagenesis of Csk in the activation loop, mutant shows slightly decreased activity compared to the wild-type enzyme
S381A
-
site-directed mutagenesis, reduced activity with substrates poly(Glu4-Tyr) and [kdSrc kinase]-L-tyrosine compared to the wild-type enzyme
S578P
missense mutation in the SH1 domain, cT1895->C
SW445P
mutation causes constitutive activation
T336A
-
site-directed mutagenesis of Csk in the activation loop, mutant shows increased activity compared to the wild-type enzyme
T342A
-
site-directed mutagenesis of Csk in the activation loop, mutant shows decreased activity compared to the wild-type enzyme
T345A
-
site-directed mutagenesis of Csk in the activation loop, mutant shows decreased activity compared to the wild-type enzyme
T478S
-
the JAK1 mutation is associated with acute myelogenous leukemia
T495R
naturally occuring mutation in kinase ABL1 of chronic myeloid leukemia patients
V299L
naturally occuring mutation in kinase ABL1 of chronic myeloid leukemia patients
V617F/C618R
the mutation is associated with polycythemia vera
V623A
-
the JAK1 mutation is associated with acute myelogenous leukemia
V881A
-
mutation is sufficient to support growth and downstream signaling at high concentrations of 2-(1,1-dimethylethyl)-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinolin-7-one, i.e. JAK inhibitor-I
W188A
-
the mutant shows increased binding to phosphorylation sites of substrates but reduced phosphorylation activity compared to the wild-type enzyme, especially with substrate poly(Glu4-Tyr)
W188F
-
the mutant shows increased binding to phosphorylation sites of substrates but reduced phosphorylation activity compared to the wild-type enzyme, especially with substrate poly(Glu4-Tyr)
Y223A
-
site-directed mutagenesis of the SH3 domain tyrosine of Btk, the mutant is not phosphorylated
Y315A
-
site-directed mutagenesis, activity is similar to the wild-type ZAP-70
Y315F
-
site-directed mutagenesis, inactive ZAP-70 mutant
Y319A
-
site-directed mutagenesis, activity is similar to the wild-type ZAP-70
Y319F
-
site-directed mutagenesis, inactive ZAP-70 mutant
Y394F
-
Lck F394 mutant cells show reduced tyrosine phosphorylation of the enzyme, expression of recombinant wild-type Lck in the mutant cells increases the autophosphorylation activity 3fold
Y402F
-
site-directed mutagenesis, mutation leads to increase in phosphorylation sites on the substrate FGFR3
Y505F
-
constitutively active Lck mutant, effect on recombinant Kv1.3 current amplitude and O2 sensitivity, overexpressing LckY505F decreased Kv1.3 current from 2.5±0.3 nA to 2.2±0.2 nA, overview
Y511A
-
site-directed mutagenesis of Src, the mutant enzyme shows reduced interaction with the Csk and reduced inactivation by Csk
Y511F
-
site-directed mutagenesis of Src, the mutant enzyme shows reduced slightly interaction with the Csk and reduced inactivation by Csk
Y511I
-
site-directed mutagenesis of Src, the mutant enzyme shows reduced interaction with the Csk and reduced inactivation by Csk
Y511L
-
site-directed mutagenesis of Src, the mutant enzyme shows reduced interaction with the Csk and reduced inactivation by Csk
Y511W
-
site-directed mutagenesis of Src, the mutant enzyme shows reduced slightly interaction with the Csk and reduced inactivation by Csk
Y530F
-
site-directed mutagenesis, a constitutively active mutant
Y531F
-
coexpression of FynY531F, SH2-defective R176K, and SH3-defective P134K mutants, but not K299M, with TCGAP enhance tyrosine phosphorylation of TCGAP
Y551E
in complex with inhibitor dasatinib, crystal structure
Y551F
-
site-directed mutagenesis, the mutant enzyme cannot be activated by autophosphorylation at Y551, and shows about 10fold reduced activation and activity compared to the wild-type enzyme
Y918H
-
mutation is sufficient to support growth and downstream signaling at high concentrations of 2-(1,1-dimethylethyl)-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinolin-7-one, i.e. JAK inhibitor-I
K273R
mutant protein is unable to transfer the gamma-phosphate of ATP but able to bind 8-azido-ATP with an efficiency similar to that of wild-type pp56lck
W1038G/E1046A
site-directed mutagenesis, an inactive dominant-negative mutant, construction of transgenic mice, heterologous mutants show reduced enzyme activity and an unaltered phenotype, overview
W1038G/E1046R
site-directed mutagenesis, an inactive dominant-negative mutant, construction of transgenic mice, heterologous mutants show reduced enzyme activity and an unaltered phenotype, overview
E255K
-
naturally occuring Abl mutant, the mutant is inhibitor imatinib-resistant
E255K
naturally occuring mutation in kinase ABL1 of chronic myeloid leukemia patients
H396P
-
naturally occurring mutation in the BCR/ABL kinase leading to resistance against inhibitor imatinib mesylate in cell culture in vitro
H396P
-
a naturally occuring Abl activation loop mutant
H396P
naturally occuring mutation in kinase ABL1 of chronic myeloid leukemia patients
K295M
-
a catalytically inactive mutant Src
K295M
-
site-directed mutagenesis, inactive Src mutant
L145P
-
coiled-coil mutation activates the enzyme
L145P
-
site-directed mutagenesis, mutation in the first coiled-coil motif, mutation leads to growth arrest of yeast cells
Q252H
-
naturally occuring Abl mutant, the mutant is inhibitor imatinib-resistant
Q252H
naturally occuring mutation in kinase ABL1 of chronic myeloid leukemia patients
R283A
-
site-directed mutagenesis of Csk, the mutant enzyme shows highly reduced interaction with the Src substrate, and slightly reduced activity with the polyEY substrate
R283A
-
site-directed mutagenesis of Csk, the mutant enzyme shows reduced interaction with the Src substrate
R288W
missense mutation in the SH2 domain, cC1026->T
R288W
mutant, residual kinase activity is present
R544S
missense mutation in the SH1 domain, cG1796->C
R544S
mutant, residual kinase activity is present
S280A
-
site-directed mutagenesis, reduced activity with substrates poly(Glu4-Tyr) and [kdSrc kinase]-L-tyrosine compared to the wild-type enzyme
S280A
-
site-directed mutagenesis of Csk, the mutant enzyme shows reduced interaction with the Src substrate
T315I
-
naturally occurring mutation in the BCR/ABL kinase leading to resistance against inhibitor imatinib mesylate in cell culture in vitro
T315I
naturally occuring mutation in kinase ABL1 of chronic myeloid leukemia patients
T315I
the mutation increases enzyme activity
V617F
-
impairment of JAK2 autoregulation caused by this mutation renders the JAK2 kinase constitutively active
V617F
-
JAK2 gain-of-function mutation underlying myeloproliferative diseases
V617F
the activating JAK2mutation has been described in the majority of patients with Philadelphia chromosome-negative myeloproliferative disorders, the incidence of the JAK2V617F mutation is about 50% in both essential thrombocythemia and primary myelofibrosis and over 90% in polycythemia vera
V617F
the mutant activates downstream signaling through the signal transducers and activators of transcription, RAS/mitogen-activated protein kinase, and phosphatidylinositol 3 /AKT pathways, conferring proliferative and survival advantages in the myeloproliferative neoplasm hematopoietic progenitor cells
V617F
the mutation is found in a significant portion of patients with myeloproliferative neoplasm, results in increased JAK2 tyrosine kinase activity, leading to clonal proliferation
V617F
the mutation is responsible for the majority of breakpoint cluster region/Abelson -negative myeloproliferative disorders
V617F
the mutation leads to constitutive tyrosine phosphorylation activity and is typically associated with polycythemia vera
V617F
the mutation promotes JAK2 catalytic activation and cytokine-independent signaling
V617F
-
the mutation within the JH2 pseudokinase domain of Jak2 is present in almost all patients with polycythemia vera, as well as high percentages also in patients with essential thrombocythemia, and idiopathic myelofibrosis
Y253F
-
naturally occuring Abl mutant, the mutant is inhibitor imatinib-resistant
Y253F
naturally occuring mutation in kinase ABL1 of chronic myeloid leukemia patients
Y253H
-
naturally occurring mutation in the BCR/ABL kinase leading to resistance against inhibitor imatinib mesylate in cell culture in vitro
Y253H
naturally occuring mutation in kinase ABL1 of chronic myeloid leukemia patients
V617F
-
JAK2 gain-of-function mutation underlying myeloproliferative diseases
V617F
the mutation modulates Skp2 gene expression through the STAT transcription factors and is regarded as the major cause of myeloproliferative disorders
V617F
-
the mutation within the JH2 pseudokinase domain of Jak2 is present in almost all patients with polycythemia vera, as well as high percentages also in patients with essential thrombocythemia, and idiopathic myelofibrosis
additional information
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construction of Fyn/Yes and Wnt11 knockout mutants, activity profiling and phenotype analysis, overview
additional information
-
gene replacement knockout mutations of genes wzc and etk in strain W3110 using a one-step-inactivation PCR-based method, revealing that Wzc is not essential, but Etk is essential for polymyxin resistance, overview
additional information
loss of the phosphorylation site at Tyr531 may contribute to the transforming abilities of carboxy-terminal deletion mutants of the fyn protein
additional information
-
loss of the phosphorylation site at Tyr531 may contribute to the transforming abilities of carboxy-terminal deletion mutants of the fyn protein
additional information
mutant lacking the C-terminal noncatalytic region has about a 10fold higher kinase activity in vitro and, when expressed in HeLa cells, induces punctate actin aggregates in the cytoplasm and unusual condensation and fragmentation of nuclei, followed by apoptosis
additional information
-
construction of a Pyk2 mutant Pyk2-DELTAKIN lacking the kinase domain resulting in loss of interaction and phosphorylation activity with FGFR3
additional information
-
construction of a residue-339-deletion mutant
additional information
-
construction of a yeast tribrid system for analysis of interaction between Fyn, DNA-bound substrate, and Grb2-SH2 domain, fluorescent reporter gene assay, overview
additional information
-
construction of chimeric mutant Fes by exchanging the wild-type SH2 domain for the SH2 domains of v-Src, Fps, or p120 Ras, construction of deletion mutants lacking either the first or the second coiled-coil motifs eliminating tyrosine kinase activity and causing growth arrest of yeast cells
additional information
-
construction of mutants DSH3 and DSH2 lacking the SH3 and SH2 domains, respectively, the mutants show decreased binding to phosphorylation sites of substrates compared to the wild-type enzyme, mutant DSH2 also shows reduced phosphorylation activity
additional information
-
deletion of SH2-kinase linker residues V177-Y184 reduces the catalytic activity of Csk to 20% of wild-type enzyme activity
additional information
-
a mutated form of c-Abl, in which the N-terminal cap and two other key contacts in the autoinhibited state are deleted, exists in an extended array of the SH3, SH2, and kinase domains. This alternative conformation of Abl is likely to prolong the active state of the kinase by preventing it from returning to the autoinhibited state, overview
additional information
-
Abl-PP harbors mutations in prolines 242 and 249 in theSH2kinase linker domain, which are mutated to glutamic acid, rendering Abl in a constitutively active state
additional information
-
construction of a transcription factor TEL-Jak2 fusion chimeric protein, leading to increase in nuclear factor IkappaB and growthfactor-independent cell proliferation, overview
additional information
-
endothelial cells lacking FAK fail to form bridging complex between integrins and fibrillar chains
additional information
-
expression of siRNA of Syk or the domainant-negative Syk mutat DN-Syk in HL-60 cells leads to inhibition of phagocytosis, overview
additional information
-
impact of siRNA-mediated Brk depletion on malignant T cells constitutively expressing the kinase, Brk depletion reproducibly inhibits proliferation of all three malignant T-cell lines
additional information
-
overexpression of constitutively active Fyn Y530F mutant localized at both ends of F-actin bundles triggers stress fiber formation, gene silencing of Fyn by siRNA expression or expression of dominant negative Fyn mutant K298M inhibit actin stress fiber formation in fibroblasts
additional information
-
Syk silencing in TNP1-cells by siRNA interference leads to inhibition of lipopolysaccharide-induced responses in the cells, and to downregulation of IL-6 and IL-8 release, overview
additional information
mutant lacking the SH4 domain
additional information
-
mutations and translocations in the JAK genes leading to constitutively active JAK proteins are associated with a variety of hematopoietic malignancies, including the myeloproliferative disorders (JAK2), acute lymphoblastic leukemia (JAK2), acute myeloid leukemia (JAK2, JAK1), acute megakaryoblastic leukemia (JAK2, JAK3) and T-cell precursor acute lymphoblastic leukemia (JAK1), loss-of-function mutations of JAK3 and TYK2 lead to immunodeficiency
additional information
-
Tyk2 mutations are associated with autosomal recessive hyperimmunoglobulin E or Jobs syndrome
additional information
expression and a two-step purification procedure for the doubly tagged full-length expression construct, H6-FL-TYK-2-FLAG. In the presence of ATP and a peptide substrate, H6-FL-TYK-2-FLAG shows a marked lag in phosphopeptide product formation, while the wild-type shows no such lag. The lag can be eliminated by ATP pretreatment. The potencies of several nanomolar inhibitors are similar for TYK-2 KD and H6-FL-TYK-2-FLAG. However, these same inhibitors are about 1000 times less potent inhibiting the autophosphorylation of H6-FL-TYK-2-FLAG than they are inhibiting the phosphorylation of a peptide substrate modeled after the activation loop sequence of wild-type TYK-2
additional information
generation of mutants of the protein-tyrosine kinase pp56lck that have single amino acid substitutions within the area surrounding the conserved residue Lys-273 in subdomain II. When compared with wild-type pp56lck, these mutants display profound reductions in their phosphotransfer efficiencies and small differences in their affinities for ATP
additional information
temperature-sensitive mutants of the lck tyrosine protein kinase
additional information
-
a gain-of-function mutant fps/fes transgene, i.e. fpsMF, encoding an activated Fps/Fes variant, i.e. MFps, is constructed, tissue-specific expression in mice, mutant mice show reduced peripheral erythrocytes and accumulation of immature erythroid precursors displaying increased survival, activation of the mutant enzyme by erythropoietin and stem cell factor leads to increased STAT5A/B activation and reduced ERK1/2 phosphorylation
additional information
-
homozygous knock-out mice with mutational inactivated Fps and Fer protein-tyrosine kinases are viable and shows reduced fertility, and deregulated hematopoiesis with elevated neutrophils, erythrocytes, and platelets, but reduced overall bone marrow cellularity, overview
additional information
-
Btk-deficient bone marrow-derived macrophages secrete decreased levels of IL-10 in response to multiple TLR ligands, compared with wild-type cells, overview
additional information
-
construction of Fyn brain knockout mice, brain-derived neurotrophic factor BDNF-induced TrkB, Akt, and PLCgamma phosphorylation is affected in Fyn knock-out neurons, phenotype, overview
additional information
-
Csk is essential for mouse embryonic development, Csk knock-out mice dye at early stages of embryogenesis around embryonic day 10, Csk deficiency in mouse embryonic fibroblast cells blocks cell migration induced by lysophosphatidic acid through G protein-coupled receptors, by platelet-derived growth factor and epidermal growth factor through receptor tyrosine kinases, and by serum, molecular mechanism, phenotype, overview
additional information
-
downregulation of Abl expression by siRNA expression in NIH 3T3 cells reduces Src-mT-induced foci
additional information
-
E-selectin-induced alpha(L)beta(2) integrin-mediated rolling is abolished in syk-/- mice bone marrow, neutrophil recruitment in a thioglycollate-induced peritonitis model is almost completely inhibited, overview
additional information
-
knockout fak-/- mice show a heavily compromised phenotype with complete absence of the cardiovascular system and early embryonic lethality, enzyme-deficient endothelial cells shows reduced migration, as well as decreased cell proliferation and survival in vivo
additional information
-
PYK2-deficient phenotype with reduced vasodilatation, response to NO, and neovessel formation, detailed overview
additional information
-
Btk-deficient bone marrow-derived macrophages secrete decreased levels of IL-10 in response to multiple TLR ligands, compared with wild-type cells, overview
-
additional information
-
enzyme deletion or mutation, e.g. in a dominant negative mutant or in Lyn-deficient bone marrow-derived mast cells, prevents internalization of the organism into host cells and affects induction of inflammatory cytokines and apoptosis
additional information
mutant lacking the C-terminal noncatalytic region has about a 10fold higher kinase activity in vitro and, when expressed in HeLa cells, induces punctate actin aggregates in the cytoplasm and unusual condensation and fragmentation of nuclei, followed by apoptosis
additional information
-
siRNA Syk knockout, overview, preparation of a stem loop rat aerosolized Syk antisense-liposome complexes leading to downregulation of airway inflammatory responses, overview
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