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ARTKQTARKSTGGKAPRK(biot)G + S-adenosyl-L-methionine
ART-methyl-KQTARKSTGGKAPRK(biot)G + S-adenosyl-L-homocysteine
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S-adenosyl-L-methionine + histone (K4)
S-adenosyl-L-homocysteine + methylated histone (K4)
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S-adenosyl-L-methionine + histone H3
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S-adenosyl-L-methionine + histone H3(K4)
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S-adenosyl-L-methionine + histone L-lysine
S-adenosyl-L-homocysteine + histone N6-methyl-L-lysine
S-adenosyl-L-methionine + TAF10-K189 peptide
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S-adenosyl-L-methionine + transcriptional factor p53
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methylation of transcriptional factor p53 with the sequence LKSKKGQSTY occurs at Lys-4
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S-adenosyl-L-methionine + [androgen receptor]-L-lysine630
S-adenosyl-L-homocysteine + [androgen receptor]-N6-methyl-L-lysine630
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S-adenosyl-L-methionine + [ribosomal protein eL42]-L-lysine100
S-adenosyl-L-homocysteine + [ribosomal protein eL42]-N6-methyl-L-lysine100
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S-adenosyl-L-methionine + [ribosomal protein eL42]-L-lysine53
S-adenosyl-L-homocysteine + [ribosomal protein eL42]-N6-methyl-L-lysine53
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S-adenosyl-L-methionine + [ribosomal protein eL42]-L-lysine80
S-adenosyl-L-homocysteine + [ribosomal protein eL42]-N6-methyl-L-lysine80
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S-adenosyl-L-methionine + [Smad3 protein]-L-lysine
S-adenosyl-L-homocysteine + [Smad3 protein]-N6-methyl-L-lysine
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S-adenosyl-L-methionine + [Smad7]-L-lysine70
S-adenosyl-L-homocysteine + [Smad7]-N6-methyl-L-lysine70
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additional information
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S-adenosyl-L-methionine + histone H3(K4)
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S-adenosyl-L-methionine + histone H3(K4)
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SET7/9 only catalyzes the transfer of one methyl group to the target lysine
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S-adenosyl-L-methionine + histone L-lysine
S-adenosyl-L-homocysteine + histone N6-methyl-L-lysine
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S-adenosyl-L-methionine + histone L-lysine
S-adenosyl-L-homocysteine + histone N6-methyl-L-lysine
the wild-type SET7/9 is a monomethylase
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additional information
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methyl-transfer reaction catalyzed by SET7/9 is a typical in-line SN2 nucleophilic substitution reaction with a transition state of 70% dissociative character, transfers only one methyl group to the unmodified histone-lysine residue H3-K4
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additional information
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SET7/9 plays an essential catalytic role in significantly lowering the barrier for the methyl-transfer reaction step
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additional information
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modification of histone tails
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Breast Neoplasms
Identification of Cyproheptadine as an Inhibitor of SET Domain Containing Lysine Methyltransferase 7/9 (Set7/9) That Regulates Estrogen-Dependent Transcription.
Breast Neoplasms
SET7/9 inhibits oncogenic activities through regulation of Gli-1 expression in breast cancer.
Breast Neoplasms
SET7/9 promotes multiple malignant processes in breast cancer development via RUNX2 activation and is negatively regulated by TRIM21.
Carcinogenesis
Identification of Cyproheptadine as an Inhibitor of SET Domain Containing Lysine Methyltransferase 7/9 (Set7/9) That Regulates Estrogen-Dependent Transcription.
Carcinogenesis
Opposite Effects of SET7/9 on Apoptosis of Human Acute Myeloid Leukemia Cells and Lung Cancer Cells.
Carcinogenesis
Reduced expression of SET7/9, a histone mono-methyltransferase, is associated with gastric cancer progression.
Carcinogenesis
Set7/9 controls proliferation and genotoxic drug resistance of NSCLC cells.
Carcinoma, Hepatocellular
SET7/9 promotes hepatocellular carcinoma progression through regulation of E2F1.
Colorectal Neoplasms
Resveratrol induces p53 in colorectal cancer through SET7/9.
Diabetes Mellitus
Role of SET7/9 in the progression of ischemic renal injury in diabetic and non-diabetic rats.
Diabetes Mellitus, Type 1
Histone H2AK119 and H2BK120 Monoubiquitination Modulate SET7/9 and SUV39H1 in Type 1 Diabetes Induced Renal Fibrosis.
Diabetes Mellitus, Type 2
SET7/9 Enzyme Regulates Cytokine-induced Expression of Inducible Nitric-oxide Synthase through Methylation of Lysine 4 at Histone 3 in the Islet ? Cell.
Glioma
SET7/9 promotes H3K4me3 at lncRNA DRAIC promoter to modulate growth and metastasis of glioma.
Glomerulonephritis, IGA
Inhibition of SET Domain-Containing Lysine Methyltransferase 7/9 Ameliorates Renal Fibrosis.
Glomerulonephritis, Membranous
Inhibition of SET Domain-Containing Lysine Methyltransferase 7/9 Ameliorates Renal Fibrosis.
Infections
Trimethylation of histone H3 lysine 4 by Set1 in the lytic infection of human herpes simplex virus 1.
Insulinoma
Methyltransferase Set7/9 maintains transcription and euchromatin structure at islet-enriched genes.
Leukemia
Histone H3K4 Methyltransferases as Targets for Drug-Resistant Cancers.
Leukemia
SMYD2 lysine methyltransferase regulates leukemia cell growth and regeneration after genotoxic stress.
Leukemia
Substrate and product specificities of SET domain methyltransferases.
Leukemia, Myeloid, Acute
Opposite Effects of SET7/9 on Apoptosis of Human Acute Myeloid Leukemia Cells and Lung Cancer Cells.
Lung Neoplasms
Opposite Effects of SET7/9 on Apoptosis of Human Acute Myeloid Leukemia Cells and Lung Cancer Cells.
Lung Neoplasms
Set7/9 controls proliferation and genotoxic drug resistance of NSCLC cells.
Metabolic Diseases
Set7/9, a methyltransferase, regulates the thermogenic program during brown adipocyte differentiation through the modulation of p53 acetylation.
Neoplasm Metastasis
SET7/9 promotes H3K4me3 at lncRNA DRAIC promoter to modulate growth and metastasis of glioma.
Neoplasms
KMT Set7/9 affects genotoxic stress response via the Mdm2 axis.
Neoplasms
KMTase Set7/9 is a critical regulator of E2F1 activity upon genotoxic stress.
Neoplasms
Methylation of p53 by Set7/9 mediates p53 acetylation and activity in vivo.
Neoplasms
Methylation of SUV39H1 by SET7/9 results in heterochromatin relaxation and genome instability.
Neoplasms
Methylation-acetylation interplay activates p53 in response to DNA damage.
Neoplasms
Opposite Effects of SET7/9 on Apoptosis of Human Acute Myeloid Leukemia Cells and Lung Cancer Cells.
Neoplasms
Reduced expression of SET7/9, a histone mono-methyltransferase, is associated with gastric cancer progression.
Neoplasms
Set7/9 controls proliferation and genotoxic drug resistance of NSCLC cells.
Neoplasms
SET7/9 promotes hepatocellular carcinoma progression through regulation of E2F1.
Neoplasms
SET7/9 promotes multiple malignant processes in breast cancer development via RUNX2 activation and is negatively regulated by TRIM21.
Neoplasms
SET7/9 regulates cancer cell proliferation by influencing ?-catenin stability.
Neoplasms
Small-Molecule Inhibitors of the Protein Methyltransferase SET7/9 Identified in a High-Throughput Screen.
Neoplasms
Structural basis for the methylation site specificity of SET7/9.
Obesity
Set7/9, a methyltransferase, regulates the thermogenic program during brown adipocyte differentiation through the modulation of p53 acetylation.
Peritoneal Fibrosis
Inhibition of the H3K4 methyltransferase SET7/9 ameliorates peritoneal fibrosis.
Prostatic Neoplasms
Histone H3K4 Methyltransferases as Targets for Drug-Resistant Cancers.
Renal Insufficiency, Chronic
Histone Lysine Methylation in TGF-?1 Mediated p21 Gene Expression in Rat Mesangial Cells.
Stomach Neoplasms
Reduced expression of SET7/9, a histone mono-methyltransferase, is associated with gastric cancer progression.
Triple Negative Breast Neoplasms
Histone H3K4 Methyltransferases as Targets for Drug-Resistant Cancers.
Ureteral Obstruction
Inhibition of SET Domain-Containing Lysine Methyltransferase 7/9 Ameliorates Renal Fibrosis.
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malfunction
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SET7/9 deficiency does not affect p65 DNA binding as assessed by electrophoretic mobility shift assays, S100b-induced gene expression is decreased by SET7/9 knockdown
physiological function
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SET7/9 may act as a transcriptional cofactor of NF-kappaB p65, SET7/9 may regulate NF-kappaB-dependent genes through modifications of chromatin histone lysine at these specific gene promoters, SET7/9 is recruited to the promoters of inflammatory genes and enhances p65 recruitment to these gene promoters, SET7/9 is not involved in monocyte differentiation but affects monocyte adhesion
physiological function
methyltransferase Set9 potentiates TGF-beta signaling by targeting Smad7, an inhibitory downstream effector. Smad7 methylation promotes interaction with the E3 ligase Arkadia and, thus, ubiquitination-dependent degradation. Depletion or pharmacological inhibition of Set9 results in elevated Smad7 protein levels and inhibits TGF-beta-dependent expression of genes encoding extracellular matrix components. Lung fibrosis induced by bleomycin or Ad-TGF-beta treatment is highly compromised in Set9-deficient mice
physiological function
SET9 interacts with SMAD3, the principal mediator of TGFB1 signalling in myofibroblasts. SET9-deficient fibroblasts exhibit globally altered gene expression profiles in response to TGFB1, whilst overexpression of SET9 enhances SMAD3 transcriptional activity. SET9 facilitates nuclear import of SMAD3 and controls SMAD3 protein degradation via ubiquitylation. SET9 is broadly required for the effects of TGFB1 in diseased primary renal fibroblasts. SET9 promotes fibroblast migration into wounds, expression of extracellular matrix proteins, collagen contractility and myofibroblast differentiation. SET9 is recruited to the alpha-smooth muscle actin gene in response to TGFB1
physiological function
SET9 interacts with the large subunit ribosomal protein, eL42. The N-terminal MORN domain of SET9 is essential for its interaction with eL42. SET9 methylates eL42 at Lys53, Lys80 and Lys100. SET9-mediated methylation of eL42 enhances global translation
physiological function
Set9 methylates the nuclear and cytoplasmic androgen receptor. Set9 overexpression potentiates androgen receptor-mediated transactivation of the probasin promoter, whereas Set9 depletion inhibits androgen receptor activity and target gene expression. Chromatin occupancy of Set9 at androgen response elements is androgen dependent, and associated with methylated histone H3K4 chromatin activation marks and p300/CBP associated factor acetyltransferase recruitment. Set9 depletion increases the histone H3K9-dimethyl repressive mark at androgen response elements and reduces histone activation marks and occupancy of p300/CBP associated factor. K630A mutation of the androgen receptor reduces amino- and carboxy-terminal interaction in Set9-intact cells, whereas amino- and carboxy-terminal interaction for wild-type androgen receptor is reduced upon Set9 depletion
physiological function
SET9 promotes HIF-1alpha protein stability in hypoxia and enhances HIF-1 mediated glycolytic gene transcription. SET9 interacts with HIF-1alpha and promotes HIF-1alpha protein stability in hypoxia. Silencing SET9 by siRNA reduces HIF-1alpha protein stability in hypoxia, and attenuates the hypoxic induction of HIF-1 target genes mediating hypoxic glycolysis. SET9 is enriched at the hypoxia response elements within promoters of the HIF-1-responsive glycolytic genes. Silencing SET9 reduces HIF-1alpha levels at these HREs in hypoxia, thereby attenuating HIF-1-mediated gene transcription. Silencing SET9 reduces hypoxia-induced glycolysis and inhibits cell viability of hypoxic cancer cells
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Hu, P.; Zhang, Y.
Catalytic mechanism and product specificity of the histone lysine methyltransferase SET7/9: an ab initio QM/MM-FE study with multiple initial structures
J. Am. Chem. Soc.
128
1272-1278
2006
Homo sapiens
brenda
Hu, P.; Zhang, Y.
Ab initio quantum mechanical/molecular mechanical molecular dynamics simulation of enzyme catalysis: the case of histone lysine methyltransferase SET7/9
J. Phys. Chem. B
111
3758-3764
2007
Homo sapiens
brenda
Mai, A.; Cheng, D.; Bedford, M.T.; Valente, S.; Nebbioso, A.; Perrone, A.; Brosch, G.; Sbardella, G.; De Bellis, F.; Miceli, M.; Altucci, L.
Epigenetic multiple ligands: mixed histone/protein methyltransferase, acetyltransferase, and class III deacetylase (sirtuin) inhibitors
J. Med. Chem.
51
2279-2290
2008
Homo sapiens
brenda
Zhang, X.; Bruice, T.C.
Mechanism of product specificity of AdoMet methylation catalyzed by lysine methyltransferases: transcriptional factor p53 methylation by histone lysine methyltransferase SET7/9
Biochemistry
47
2743-2748
2008
Homo sapiens
brenda
Li, Y.; Reddy, M.A.; Miao, F.; Shanmugam, N.; Yee, J.K.; Hawkins, D.; Ren, B.; Natarajan, R.
Role of the histone H3 lysine 4 methyltransferase, SET7/9, in the regulation of NF-kappaB-dependent inflammatory genes. Relevance to diabetes and inflammation
J. Biol. Chem.
283
26771-26781
2008
Homo sapiens
brenda
Zhang, X.; Bruice, T.C.
Enzymatic mechanism and product specificity of SET-domain protein lysine methyltransferases
Proc. Natl. Acad. Sci. USA
105
5728-5732
2008
Homo sapiens
brenda
Yao, J.; Chu, Y.; An, R.; Guo, H.
Understanding product specificity of protein lysine methyltransferases from QM/MM molecular dynamics and free energy simulations: the effects of mutation on SET7/9 beyond the Tyr/Phe switch
J. Chem. Inf. Model.
52
449-456
2012
Homo sapiens (Q8WTS6)
brenda
Georgieva, P.; Himo, F.
Quantum chemical modeling of enzymatic reactions: the case of histone lysine methyltransferase
J. Comput. Chem.
31
1707-1714
2010
Homo sapiens (Q8WTS6)
brenda
Guitot, K.; Scarabelli, S.; Drujon, T.; Bolbach, G.; Amoura, M.; Burlina, F.; Jeltsch, A.; Sagan, S.; Guianvarch, D.
Label-free measurement of histone lysine methyltransferases activity by matrix-assisted laser desorption/ionization time-of-flight mass spectrometry
Anal. Biochem.
456
25-31
2014
Homo sapiens (Q8WTS6)
brenda
Liu, Q.; Geng, H.; Xue, C.; Beer, T.; Qian, D.
Functional regulation of hypoxia inducible factor-1alpha by SET9 lysine methyltransferase
Biochim. Biophys. Acta
1853
881-891
2015
Homo sapiens (Q8WTS6)
brenda
Mahesh, A.; Khan, M.; Govindaraju, G.; Verma, M.; Awasthi, S.; Chavali, P.; Chavali, S.; Rajavelu, A.; Dhayalan, A.
SET7/9 interacts and methylates the ribosomal protein, eL42 and regulates protein synthesis
Biochim. Biophys. Acta
1867
118611
2020
Homo sapiens (Q8WTS6)
brenda
Elkouris, M.; Kontaki, H.; Stavropoulos, A.; Antonoglou, A.; Nikolaou, K.; Samiotaki, M.; Szantai, E.; Saviolaki, D.; Brown, P.; Sideras, P.; Panayotou, G.; Talianidis, I.
SET9-mediated regulation of TGF-beta signaling links protein methylation to pulmonary fibrosis
Cell Rep.
15
2733-2744
2016
Mus musculus (Q8VHL1)
brenda
Shuttleworth, V.; Gaughan, L.; Nawafa, L.; Mooney, C.; Cobb, S.; Sheerin, N.; Logan, I.
The methyltransferase SET9 regulates TGFB1 activation of renal fibroblasts via interaction with SMAD3
J. Cell Sci.
131
jcs207761
2018
Mus musculus (Q8VHL1)
brenda
Ko, S.; Ahn, J.; Song, C.; Kim, S.; Knapczyk-Stwora, K.; Chatterjee, B.
Lysine methylation and functional modulation of androgen receptor by set9 methyltransferase
Mol. Endocrinol.
25
433-444
2011
Homo sapiens (Q8WTS6)
brenda