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Literature summary for 2.7.10.2 extracted from

  • Anastasiadou, E.; Schwaller, J.
    Role of constitutively activated protein tyrosine kinases in malignant myeloproliferative disorders: an update (2003), Curr. Opin. Hematol., 10, 40-48.
    View publication on PubMed

Application

Application Comment Organism
pharmacology ABL protein tyrosine kinase is a target for treatment of chronic myeloid leukemia with imatinib mesylate, synergistic with AG-490, an inhibitor of JAK2 tyrosine kinase signaling Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
genetic analysis of mutations causing cell cycle deregulation, e.g. in mice lacking cyclin-D2, heterozygous D2+/- mice are resistant to BCR/ABL-induced proliferation, overview Mus musculus
genetic analysis of mutations causing myeloid malignancies Homo sapiens

Protein Variants

Protein Variants Comment Organism
E225K naturally occurring mutation in the BCR/ABL kinase leading to resistance against inhibitor imatinib mesylate in vivo and in cell culture in vitro Homo sapiens
E225V naturally occurring mutation in the BCR/ABL kinase leading to resistance against inhibitor imatinib mesylate in cell culture in vitro Homo sapiens
H396P naturally occurring mutation in the BCR/ABL kinase leading to resistance against inhibitor imatinib mesylate in cell culture in vitro Homo sapiens
T315I naturally occurring mutation in the BCR/ABL kinase leading to resistance against inhibitor imatinib mesylate in cell culture in vitro Homo sapiens
Y253H naturally occurring mutation in the BCR/ABL kinase leading to resistance against inhibitor imatinib mesylate in cell culture in vitro Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
AG-490 inhibits JAK2 tyrosine kinase Homo sapiens
imatinib mesylate 2-phenylaminopyrimidine derivate, i.e. CGP-57148, inhibits BCR/ABL kinase, used in antityrosine kinase therapy of myeloid leukemia Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
additional information Homo sapiens 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 ?
-
?
additional information Mus musculus 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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?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Mus musculus
-
-
-

Posttranslational Modification

Posttranslational Modification Comment Organism
phosphoprotein tyrosine autophosphorylation of BCR/ABL kinase Mus musculus
phosphoprotein tyrosine autophosphorylation of BCR/ABL kinase at Tyr177 Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
bone marrow
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Mus musculus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
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, 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 Homo sapiens ?
-
?
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 Mus musculus ?
-
?
additional information the BCR/ABL kinase performs tyrosine autophosphorylation, mechanism Mus musculus ?
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?
additional information the BCR/ABL kinase performs tyrosine autophosphorylation, mechanism Homo sapiens ?
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?

Synonyms

Synonyms Comment Organism
Abl protein tyrosine kinase
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Homo sapiens
BCR/ABL kinase
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Mus musculus
BCR/ABL kinase
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Homo sapiens
JAK2 tyrosine kinase
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Homo sapiens
Protein tyrosine kinase
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Mus musculus
Protein tyrosine kinase
-
Homo sapiens
PTK
-
Mus musculus
PTK
-
Homo sapiens