EHMT2

Summary

Gene Symbol: EHMT2
Description: euchromatic histone lysine methyltransferase 2
Alias: BAT8, C6orf30, G9A, GAT8, KMT1C, NG36, histone-lysine N-methyltransferase EHMT2, G9A histone methyltransferase, H3-K9-HMTase 3, HLA-B associated transcript 8, ankyrin repeat-containing protein, euchromatic histone-lysine N-methyltransferase 2, histone H3-K9 methyltransferase 3, histone-lysine N-methyltransferase, H3 lysine-9 specific 3, lysine N-methyltransferase 1C
Species: human
Products:     EHMT2

Top Publications

  1. Huang J, Dorsey J, Chuikov S, Pérez Burgos L, Zhang X, Jenuwein T, et al. G9a and Glp methylate lysine 373 in the tumor suppressor p53. J Biol Chem. 2010;285:9636-41 pubmed publisher
    ..describe a novel lysine methylation site in p53 that is carried out by two homologous histone methyltransferases, G9a and Glp. G9a and Glp specifically methylate p53 at Lys(373), resulting mainly in dimethylation...
  2. Nishio H, Walsh M. CCAAT displacement protein/cut homolog recruits G9a histone lysine methyltransferase to repress transcription. Proc Natl Acad Sci U S A. 2004;101:11257-62 pubmed
    ..Here, we report that CDP/cut interacts with a histone lysine methyltransferase (HKMT), G9a, in vivo and in vitro. The deletion of the cut repeats within CDP/cut abrogates the interaction with G9a...
  3. de Vogel S, Wouters K, Gottschalk R, Van Schooten F, de Goeij A, De Bruine A, et al. Genetic variants of methyl metabolizing enzymes and epigenetic regulators: associations with promoter CpG island hypermethylation in colorectal cancer. Cancer Epidemiol Biomarkers Prev. 2009;18:3086-96 pubmed publisher
    ..metabolizing enzymes (MTHFR, MTR, and MTRR), DNA methyltransferase DNMT3b, and histone methyltransferases (EHMT1, EHMT2, and PRDM2), with colorectal cancers, with or without the CpG island methylator phenotype (CIMP), MLH1 ..
  4. Artal Martinez de Narvajas A, Gomez T, Zhang J, Mann A, Taoda Y, Gorman J, et al. Epigenetic regulation of autophagy by the methyltransferase G9a. Mol Cell Biol. 2013;33:3983-93 pubmed publisher
    ..Here we show that the methyltransferase G9a coordinates the transcriptional activation of key regulators of autophagosome formation by remodeling the chromatin ..
  5. Esteve P, Chin H, Smallwood A, Feehery G, Gangisetty O, Karpf A, et al. Direct interaction between DNMT1 and G9a coordinates DNA and histone methylation during replication. Genes Dev. 2006;20:3089-103 pubmed
    ..During cell division, DNMT1 maintains the DNA methylation pattern of the newly synthesized daughter strand, while G9a methylates H3K9...
  6. Roopra A, Qazi R, Schoenike B, Daley T, Morrison J. Localized domains of G9a-mediated histone methylation are required for silencing of neuronal genes. Mol Cell. 2004;14:727-38 pubmed
    ..Here we report that NRSF recruits the histone methylase G9a to silence NRSF target genes in nonneuronal cells...
  7. Chin H, Esteve P, Pradhan M, Benner J, Patnaik D, Carey M, et al. Automethylation of G9a and its implication in wider substrate specificity and HP1 binding. Nucleic Acids Res. 2007;35:7313-23 pubmed
    ..b>G9a methyltransferase is a euchromatic histone H3 lysine 9 methyltransferase...
  8. Kuppuswamy M, Vijayalingam S, Zhao L, Zhou Y, Subramanian T, Ryerse J, et al. Role of the PLDLS-binding cleft region of CtBP1 in recruitment of core and auxiliary components of the corepressor complex. Mol Cell Biol. 2008;28:269-81 pubmed
    ..consists of enzymatic constituents such as histone deacetylases (HDAC1/2), histone methyl transferases (HMTases; G9a and GLP), and the lysine-specific demethylase (LSD1)...
  9. Tachibana M, Sugimoto K, Nozaki M, Ueda J, Ohta T, Ohki M, et al. G9a histone methyltransferase plays a dominant role in euchromatic histone H3 lysine 9 methylation and is essential for early embryogenesis. Genes Dev. 2002;16:1779-91 pubmed
    ..We recently identified a mammalian histone methyltransferase (HMTase), G9a, which has strong HMTase activity towards H3-K9 in vitro...

More Information

Publications82

  1. Collins R, Tachibana M, Tamaru H, Smith K, Jia D, Zhang X, et al. In vitro and in vivo analyses of a Phe/Tyr switch controlling product specificity of histone lysine methyltransferases. J Biol Chem. 2005;280:5563-70 pubmed publisher
    ..vivo and found that a Phe at the position equivalent to Phe(281) of Neurospora crassa DIM-5 or Phe(1205) of human G9a allows the enzyme to perform di and tri-methylation, whereas a Tyr at this position is restrictive, inhibiting tri-..
  2. Dong C, Wu Y, Yao J, Wang Y, Yu Y, Rychahou P, et al. G9a interacts with Snail and is critical for Snail-mediated E-cadherin repression in human breast cancer. J Clin Invest. 2012;122:1469-86 pubmed publisher
    ..Further, Snail interacted with G9a, a major euchromatin methyltransferase responsible for H3K9me2, and recruited G9a and DNA methyltransferases to the ..
  3. Tachibana M, Sugimoto K, Fukushima T, Shinkai Y. Set domain-containing protein, G9a, is a novel lysine-preferring mammalian histone methyltransferase with hyperactivity and specific selectivity to lysines 9 and 27 of histone H3. J Biol Chem. 2001;276:25309-17 pubmed
    ..Here we show that a SET domain-containing protein, G9a, is a novel mammalian lysine-preferring HMTase...
  4. Yuan Y, Tang A, Castoreno A, Kuo S, Wang Q, Kuballa P, et al. Gossypol and an HMT G9a inhibitor act in synergy to induce cell death in pancreatic cancer cells. Cell Death Dis. 2013;4:e690 pubmed publisher
    The histone methyltransferase G9a is overexpressed in a variety of cancer types, including pancreatic adenocarcinoma, and promotes tumor invasiveness and metastasis...
  5. Maze I, Covington H, Dietz D, LaPlant Q, Renthal W, Russo S, et al. Essential role of the histone methyltransferase G9a in cocaine-induced plasticity. Science. 2010;327:213-6 pubmed publisher
    ..we identified an essential role for histone 3 lysine 9 (H3K9) dimethylation and the lysine dimethyltransferase G9a in cocaine-induced structural and behavioral plasticity...
  6. Cho H, Kelly J, Hayami S, Toyokawa G, Takawa M, Yoshimatsu M, et al. Enhanced expression of EHMT2 is involved in the proliferation of cancer cells through negative regulation of SIAH1. Neoplasia. 2011;13:676-84 pubmed
    b>EHMT2 is a histone lysine methyltransferase localized in euchromatin regions and acting as a corepressor for specific transcription factors...
  7. Rathert P, Dhayalan A, Murakami M, Zhang X, Tamas R, Jurkowska R, et al. Protein lysine methyltransferase G9a acts on non-histone targets. Nat Chem Biol. 2008;4:344-6 pubmed publisher
    By methylation of peptide arrays, we determined the specificity profile of the protein methyltransferase G9a. We show that it mostly recognizes an Arg-Lys sequence and that its activity is inhibited by methylation of the arginine residue...
  8. Ogawa H, Ishiguro K, Gaubatz S, Livingston D, Nakatani Y. A complex with chromatin modifiers that occupies E2F- and Myc-responsive genes in G0 cells. Science. 2002;296:1132-6 pubmed
    ..The E2F-6 complex preferentially occupies target promoters in G0 cells rather than in G1 cells. These data suggest that these chromatin modifiers contribute to silencing of E2F- and Myc-responsive genes in quiescent cells. ..
  9. Lee J, Kim Y, Kim I, Kim B, Choi H, Lee J, et al. Negative regulation of hypoxic responses via induced Reptin methylation. Mol Cell. 2010;39:71-85 pubmed publisher
    ..Reptin, a chromatin-remodeling factor, is methylated at lysine 67 in hypoxic conditions by the methyltransferase G9a. Methylated Reptin binds to the promoters of a subset of hypoxia-responsive genes and negatively regulates ..
  10. Kim Y, Kim Y, Kim D, Lee J, Song J, Kim H, et al. BIX-01294 induces autophagy-associated cell death via EHMT2/G9a dysfunction and intracellular reactive oxygen species production. Autophagy. 2013;9:2126-39 pubmed publisher
    ..assay, and identified BIX-01294 (BIX), a selective inhibitor of euchromatic histone-lysine N-methyltransferase 2 (EHMT2), as a strong autophagy inducer...
  11. Fang S, Miao J, Xiang L, Ponugoti B, Treuter E, Kemper J. Coordinated recruitment of histone methyltransferase G9a and other chromatin-modifying enzymes in SHP-mediated regulation of hepatic bile acid metabolism. Mol Cell Biol. 2007;27:1407-24 pubmed
    ..The histone methyltransferase G9a, but not SUV39, was colocalized with SHP in the nucleus and directly interacted with SHP in vitro...
  12. Gyory I, Wu J, Fejer G, Seto E, Wright K. PRDI-BF1 recruits the histone H3 methyltransferase G9a in transcriptional silencing. Nat Immunol. 2004;5:299-308 pubmed
    ..promoter in the osteosarcoma cell line U2OS through recruitment of the histone H3 lysine methyltransferase G9a. G9a is recruited only when in a complex with PRDI-BF1...
  13. Nagano T, Mitchell J, Sanz L, Pauler F, Ferguson Smith A, Feil R, et al. The Air noncoding RNA epigenetically silences transcription by targeting G9a to chromatin. Science. 2008;322:1717-20 pubmed publisher
    ..We show that Air interacts with the Slc22a3 promoter chromatin and the H3K9 histone methyltransferase G9a in placenta...
  14. Son H, Kim J, Hahn Y, Seo S. Negative regulation of JAK2 by H3K9 methyltransferase G9a in leukemia. Mol Cell Biol. 2012;32:3681-94 pubmed publisher
    ..Here, we report that the H3K9 methyltransferase G9a negatively regulated JAK2 transcription in histone methyltransferase activity and in a YY1-dependent manner during ..
  15. Ding J, Li T, Wang X, Zhao E, Choi J, Yang L, et al. The histone H3 methyltransferase G9A epigenetically activates the serine-glycine synthesis pathway to sustain cancer cell survival and proliferation. Cell Metab. 2013;18:896-907 pubmed publisher
    ..Here we show that the histone H3 lysine 9 (H3K9) methyltransferase G9A is required for maintaining the pathway enzyme genes in an active state marked by H3K9 monomethylation and for the ..
  16. Chin H, Pradhan M, Esteve P, Patnaik D, Evans T, Pradhan S. Sequence specificity and role of proximal amino acids of the histone H3 tail on catalysis of murine G9A lysine 9 histone H3 methyltransferase. Biochemistry. 2005;44:12998-3006 pubmed
    The activity of recombinant murine G9a toward lysine 9 of histone H3 was investigated...
  17. Chen M, Hua K, Kao H, Chi C, Wei L, Johansson G, et al. H3K9 histone methyltransferase G9a promotes lung cancer invasion and metastasis by silencing the cell adhesion molecule Ep-CAM. Cancer Res. 2010;70:7830-40 pubmed publisher
    b>G9a is a mammalian histone methyltransferase that contributes to the epigenetic silencing of tumor suppressor genes...
  18. Trojer P, Li G, Sims R, Vaquero A, Kalakonda N, Boccuni P, et al. L3MBTL1, a histone-methylation-dependent chromatin lock. Cell. 2007;129:915-28 pubmed
    ..Consistently, L3MBTL1 was found to negatively regulate the expression of a subset of genes regulated by E2F, a factor that interacts with Rb. ..
  19. Ueda J, Tachibana M, Ikura T, Shinkai Y. Zinc finger protein Wiz links G9a/GLP histone methyltransferases to the co-repressor molecule CtBP. J Biol Chem. 2006;281:20120-8 pubmed
    b>G9a is a SET-domain mammalian histone methyltransferase responsible for mono- and dimethylation of lysine 9 in histone H3 (H3K9) at euchromatic regions...
  20. El Gazzar M, Yoza B, Chen X, Hu J, Hawkins G, McCall C. G9a and HP1 couple histone and DNA methylation to TNFalpha transcription silencing during endotoxin tolerance. J Biol Chem. 2008;283:32198-208 pubmed publisher
    ..analysis demonstrated that, in tolerant cells, TNFalpha promoter is bound by the H3K9 histone methyltransferase G9a which dimethylates H3K9 and creates a platform for HP1 binding, leading to the recruitment of the DNA ..
  21. Shi Y, Sawada J, Sui G, Affar E, Whetstine J, Lan F, et al. Coordinated histone modifications mediated by a CtBP co-repressor complex. Nature. 2003;422:735-8 pubmed
    ..These findings identify a molecular mechanism by which CtBP mediates transcriptional repression and provide insight into CtBP participation in oncogenesis. ..
  22. Kondo Y, Shen L, Ahmed S, Boumber Y, Sekido Y, Haddad B, et al. Downregulation of histone H3 lysine 9 methyltransferase G9a induces centrosome disruption and chromosome instability in cancer cells. PLoS ONE. 2008;3:e2037 pubmed publisher
    ..We studied RNAi-based inhibition (knockdown, KD) of 2 different H3K9 HMTs, SUV39H1 and G9a. Knockdown of the 2 HMTs in PC3 cancer cell line markedly inhibited cell growth and caused profound morphological ..
  23. Duan Z, Zarebski A, Montoya Durango D, Grimes H, Horwitz M. Gfi1 coordinates epigenetic repression of p21Cip/WAF1 by recruitment of histone lysine methyltransferase G9a and histone deacetylase 1. Mol Cell Biol. 2005;25:10338-51 pubmed
    ..Here we show that Gfi1 recruits the histone lysine methyltransferase G9a and the histone deacetylase 1 (HDAC1) in order to modify the chromatin of genes targeted for repression by Gfi1...
  24. Bittencourt D, Wu D, Jeong K, Gerke D, Herviou L, Ianculescu I, et al. G9a functions as a molecular scaffold for assembly of transcriptional coactivators on a subset of glucocorticoid receptor target genes. Proc Natl Acad Sci U S A. 2012;109:19673-8 pubmed publisher
    Histone H3 lysine-9 methyltransferase G9a/EHMT2/KMT1C is a key corepressor of gene expression...
  25. Brown S, Campbell R, Sanderson C. Novel NG36/G9a gene products encoded within the human and mouse MHC class III regions. Mamm Genome. 2001;12:916-24 pubmed
    Previous annotation of the Class III region of the human Major Histocompatibility Complex (MHC) depicts NG36 as an independent gene, which lies immediately centromeric to the G9a gene...
  26. Schaefer A, Sampath S, Intrator A, Min A, Gertler T, Surmeier D, et al. Control of cognition and adaptive behavior by the GLP/G9a epigenetic suppressor complex. Neuron. 2009;64:678-91 pubmed publisher
    ..Here we demonstrate that the histone methyltransferase complex GLP/G9a controls cognition and adaptive responses in a region-specific fashion in the adult brain...
  27. Collins R, Northrop J, Horton J, Lee D, Zhang X, Stallcup M, et al. The ankyrin repeats of G9a and GLP histone methyltransferases are mono- and dimethyllysine binding modules. Nat Struct Mol Biol. 2008;15:245-50 pubmed publisher
    Histone modifications have important roles in transcriptional control, mitosis and heterochromatin formation. G9a and G9a-like protein (GLP) are euchromatin-associated methyltransferases that repress transcription by mono- and ..
  28. Chang Y, Sun L, Kokura K, Horton J, Fukuda M, Espejo A, et al. MPP8 mediates the interactions between DNA methyltransferase Dnmt3a and H3K9 methyltransferase GLP/G9a. Nat Commun. 2011;2:533 pubmed publisher
    ..Here we show that G9a or G9a-like protein (GLP) dimethylate the amino-terminal lysine 44 (K44) of mouse Dnmt3a (equivalent to K47 of ..
  29. Lee D, Northrop J, Kuo M, Stallcup M. Histone H3 lysine 9 methyltransferase G9a is a transcriptional coactivator for nuclear receptors. J Biol Chem. 2006;281:8476-85 pubmed
    Methylation of Lys-9 of histone H3 has been associated with repression of transcription. G9a is a histone H3 Lys-9 methyltransferase localized in euchromatin and acts as a corepressor for specific transcription factors...
  30. Purcell D, Khalid O, Ou C, Little G, Frenkel B, Baniwal S, et al. Recruitment of coregulator G9a by Runx2 for selective enhancement or suppression of transcription. J Cell Biochem. 2012;113:2406-14 pubmed publisher
    ..cell line that conditionally expressed Runx2 in response to doxycycline treatment, we identified and characterized G9a, a histone methyltransferase, as a novel regulator for Runx2 activity. G9a function was locus-dependent...
  31. Epsztejn Litman S, Feldman N, Abu Remaileh M, Shufaro Y, Gerson A, Ueda J, et al. De novo DNA methylation promoted by G9a prevents reprogramming of embryonically silenced genes. Nat Struct Mol Biol. 2008;15:1176-1183 pubmed publisher
    ..also called Pou5f1) undergoes postimplantation silencing in a process mediated by the histone methyltransferase G9a. Microarray analysis now shows that this enzyme may operate as a master regulator that inactivates numerous early-..
  32. Trojer P, Zhang J, Yonezawa M, Schmidt A, Zheng H, Jenuwein T, et al. Dynamic Histone H1 Isotype 4 Methylation and Demethylation by Histone Lysine Methyltransferase G9a/KMT1C and the Jumonji Domain-containing JMJD2/KDM4 Proteins. J Biol Chem. 2009;284:8395-405 pubmed publisher
    ..Here we report that the euchromatic histone lysine methyltransferase G9a/KMT1C mediates H1...
  33. Wang Y, Zhang J, Su Y, Shen Y, Jiang D, Hou Y, et al. G9a regulates breast cancer growth by modulating iron homeostasis through the repression of ferroxidase hephaestin. Nat Commun. 2017;8:274 pubmed publisher
    b>G9a, a H3K9 methyltransferase, shows elevated expression in many types of human cancers, particularly breast cancer. However, the tumorigenic mechanism of G9a is still far from clear...
  34. Liu Y, Liu S, Yuan S, Yu H, Zhang Y, Yang X, et al. Chromodomain protein CDYL is required for transmission/restoration of repressive histone marks. J Mol Cell Biol. 2017;9:178-194 pubmed publisher
    ..We demonstrated that CDYL recruits histone-modifying enzymes G9a, SETDB1, and EZH2 to replication forks, leading to the addition of H3K9me2/3 and H3K27me2/3 on newly deposited ..
  35. Fang R, Barbera A, Xu Y, Rutenberg M, Leonor T, Bi Q, et al. Human LSD2/KDM1b/AOF1 regulates gene transcription by modulating intragenic H3K4me2 methylation. Mol Cell. 2010;39:222-33 pubmed publisher
    ..of the LSD2 complex reveals that LSD2 forms active complexes with euchromatic histone methyltransferases G9a and NSD3 as well as cellular factors involved in transcription elongation...
  36. Sonkar R, Powell C, Choudhury M. Benzyl butyl phthalate induces epigenetic stress to enhance adipogenesis in mesenchymal stem cells. Mol Cell Endocrinol. 2016;431:109-22 pubmed publisher
    ..01, 10 ?M BBP; P < 0.001, 50 ?M BBP) and histone methyltransferases, SETDB1 (P < 0.01) and G9a (P < 0.01), were significantly downregulated by BBP exposure...
  37. Liu C, Hua K, Li K, Kao H, Hong R, Ko J, et al. Histone Methyltransferase G9a Drives Chemotherapy Resistance by Regulating the Glutamate-Cysteine Ligase Catalytic Subunit in Head and Neck Squamous Cell Carcinoma. Mol Cancer Ther. 2017;16:1421-1434 pubmed publisher
    ..Histone methyltransferase G9a has recently been shown to be abundantly expressed in HNSCC, and is required to maintain the malignant phenotype...
  38. Berg M, Hoffman K, Genereaux J, Mian S, Trussler R, Haniford D, et al. Evolving Mistranslating tRNAs Through a Phenotypically Ambivalent Intermediate in Saccharomyces cerevisiae. Genetics. 2017;206:1865-1879 pubmed publisher
    ..The second tRNASerUGG variant, with a G9A mutation, had minimal effect on cell growth, was relatively stable in cells, and gave rise to less of a heat shock ..
  39. Ow J, Palanichamy Kala M, Rao V, Choi M, Bharathy N, Taneja R. G9a inhibits MEF2C activity to control sarcomere assembly. Sci Rep. 2016;6:34163 pubmed publisher
    In this study, we demonstrate that the lysine methyltransferase G9a inhibits sarcomere organization through regulation of the MEF2C-HDAC5 regulatory axis. Sarcomeres are essential for muscle contractile function...
  40. Zhang R, Judson R, Liu D, Kast J, Rossi F. The lysine methyltransferase Ehmt2/G9a is dispensable for skeletal muscle development and regeneration. Skelet Muscle. 2016;6:22 pubmed publisher
    Euchromatic histone-lysine N-methyltransferase 2 (G9a/Ehmt2) is the main enzyme responsible for the apposition of H3K9 di-methylation on histones...
  41. Renneville A, van Galen P, Canver M, McConkey M, Krill Burger J, Dorfman D, et al. EHMT1 and EHMT2 inhibition induces fetal hemoglobin expression. Blood. 2015;126:1930-9 pubmed publisher
    ..Using a small-molecule screen, we found that UNC0638, a selective inhibitor of EHMT1 and EHMT2 histone methyltransferases, induces γ-globin expression...
  42. Vilhais Neto G, Fournier M, Plassat J, Sardiu M, Saraf A, Garnier J, et al. The WHHERE coactivator complex is required for retinoic acid-dependent regulation of embryonic symmetry. Nat Commun. 2017;8:728 pubmed publisher
    ..We also identify the Rere-binding histone methyltransferase Ehmt2/G9a, as a RA coactivator controlling somite symmetry...
  43. Wang L, Dong X, Ren Y, Luo J, Liu P, Su D, et al. Targeting EHMT2 reverses EGFR-TKI resistance in NSCLC by epigenetically regulating the PTEN/AKT signaling pathway. Cell Death Dis. 2018;9:129 pubmed publisher
    ..Here, we found that an EHMT2 inhibitor, UNC0638, can significantly inhibit cell growth and induce apoptosis in EGFR-TKI-resistant NSCLC cells...
  44. Kim Y, Kim H, Lee J, Yu S, Yoon J, Lee H, et al. A genome-wide association study identified new variants associated with the risk of chronic hepatitis B. Hum Mol Genet. 2013;22:4233-8 pubmed publisher
    ..g. rs652888 on euchromatic histone-lysine-methyltransferase 2 (EHMT2, P = 7.07 × 10(-13)) and rs1419881 on transcription factor 19 (TCF19, P = 1.26 × 10(-18))...
  45. Kang K, Piao M, Ryu Y, Kang H, Chang W, Keum Y, et al. Interaction of DNA demethylase and histone methyltransferase upregulates Nrf2 in 5-fluorouracil-resistant colon cancer cells. Oncotarget. 2016;7:40594-40620 pubmed publisher
    ..a histone methyltransferase, was upregulated, leading to increased trimethylation of histone H3 lysine 4, while G9a was downregulated, leading to decreased dimethylation of histone H3 lysine 9...
  46. Han P, Li W, Yang J, Shang C, Lin C, Cheng W, et al. Epigenetic response to environmental stress: Assembly of BRG1-G9a/GLP-DNMT3 repressive chromatin complex on Myh6 promoter in pathologically stressed hearts. Biochim Biophys Acta. 2016;1863:1772-81 pubmed publisher
    ..In mice, pathological stress activates cardiomyocytes to express Brg1 (nucleosome-remodeling factor), G9a/Glp (histone methyltransferase), and Dnmt3 (DNA methyltransferase)...
  47. Zhang Y, Chen S, Laumet G, Chen H, Pan H. Nerve Injury Diminishes Opioid Analgesia through Lysine Methyltransferase-mediated Transcriptional Repression of μ-Opioid Receptors in Primary Sensory Neurons. J Biol Chem. 2016;291:8475-85 pubmed publisher
    ..G9a (encoded by Ehmt2), a histone 3 at lysine 9 methyltransferase, is a key chromatin regulator responsible for gene silencing...
  48. Zhong X, Chen X, Guan X, Zhang H, Ma Y, Zhang S, et al. Overexpression of G9a and MCM7 in oesophageal squamous cell carcinoma is associated with poor prognosis. Histopathology. 2015;66:192-200 pubmed publisher
    Histone methyltransferase G9a has been primarily understood as a co-repressor of gene expression, but it has been shown that G9a also positively regulates nuclear receptor-mediated transcription...
  49. Fiszbein A, Giono L, Quaglino A, Berardino B, Sigaut L, von Bilderling C, et al. Alternative Splicing of G9a Regulates Neuronal Differentiation. Cell Rep. 2016;14:2797-808 pubmed publisher
    Chromatin modifications are critical for the establishment and maintenance of differentiation programs. G9a, the enzyme responsible for histone H3 lysine 9 dimethylation in mammalian euchromatin, exists as two isoforms with differential ..
  50. Lee S, Kim J, Kim W, Lee Y. Hypoxic silencing of tumor suppressor RUNX3 by histone modification in gastric cancer cells. Oncogene. 2009;28:184-94 pubmed publisher
    ..Hypoxia resulted in the upregulation of G9a histone methyltransferase (HMT) and HDAC1; additionally, overexpression of G9a and HDAC1 attenuated RUNX3 expression...
  51. Wang L, Charroux B, Kerridge S, Tsai C. Atrophin recruits HDAC1/2 and G9a to modify histone H3K9 and to determine cell fates. EMBO Rep. 2008;9:555-62 pubmed publisher
    ..Here, we report that the SANT domain in RERE binds to the histone methyltransferase G9a, and that both the ELM2 and SANT domains orchestrate molecular events that lead to a stable methylation of histone ..
  52. Wu Q, Li J, Sun S, Chen X, Zhang H, Li B, et al. YAP/TAZ-mediated activation of serine metabolism and methylation regulation is critical for LKB1-deficient breast cancer progression. Biosci Rep. 2017;37: pubmed publisher
    ..Further, we speculate that YAP/TAZ in dependent of FOS may promote DNMT1 and subsequently mediate DNMT1-G9A complex involving serine metabolism and the methylation of DNA and histone...
  53. Koemans T, Kleefstra T, Chubak M, Stone M, Reijnders M, de Munnik S, et al. Functional convergence of histone methyltransferases EHMT1 and KMT2C involved in intellectual disability and autism spectrum disorder. PLoS Genet. 2017;13:e1006864 pubmed publisher
    ..Similar to the Drosophila EHMT1 ortholog, G9a, trr is required in the mushroom body for short term memory...
  54. Li F, Zeng J, Gao Y, Guan Z, Ma Z, Shi Q, et al. G9a Inhibition Induces Autophagic Cell Death via AMPK/mTOR Pathway in Bladder Transitional Cell Carcinoma. PLoS ONE. 2015;10:e0138390 pubmed publisher
    b>G9a has been reported to highly express in bladder transitional cell carcinoma (TCC) and G9a inhibition significantly attenuates cell proliferation, but the underlying mechanism is not fully understood...
  55. Liu Q, Cai X, Yang D, Chen Y, Wang Y, Shao L, et al. Cycloalkane analogues of sinefungin as EHMT1/2 inhibitors. Bioorg Med Chem. 2017;25:4579-4594 pubmed publisher
    ..9%, IC50=21.8?M for EHMT1 and 77.6%, IC50=39.6?M for EHMT2, respectively) similar to that of sinefungin (100.0%, IC50=28.4?M for EHMT1 and 79...
  56. Imai K, Togami H, Okamoto T. Involvement of histone H3 lysine 9 (H3K9) methyltransferase G9a in the maintenance of HIV-1 latency and its reactivation by BIX01294. J Biol Chem. 2010;285:16538-45 pubmed publisher
    ..Here we present evidence that histone H3 Lys(9) (H3K9) methyltransferase G9a is responsible for transcriptional repression of HIV-1 by promoting repressive dimethylation at H3K9 and for the ..
  57. Ahmad F, Dixit D, Joshi S, Sen E. G9a inhibition induced PKM2 regulates autophagic responses. Int J Biochem Cell Biol. 2016;78:87-95 pubmed publisher
    Epigenetic regulation by histone methyltransferase G9a is known to control autophagic responses...
  58. Zhang J, Gao Q, Li P, Liu X, Jia Y, Wu W, et al. S phase-dependent interaction with DNMT1 dictates the role of UHRF1 but not UHRF2 in DNA methylation maintenance. Cell Res. 2011;21:1723-39 pubmed publisher
    ..Coimmunoprecipitation experiments demonstrate that both UHRF1 and UHRF2 interact with DNMT1, DNMT3a, DNMT3b and G9a. Despite all these conserved functions, we find that UHRF2 is not able to rescue the DNA methylation defect in ..
  59. Shan C, Wang J, Xu K, Chen H, Yue J, Andrews S, et al. A histone H3K9M mutation traps histone methyltransferase Clr4 to prevent heterochromatin spreading. elife. 2016;5: pubmed publisher
    ..We further determined the crystal structure of an H3K9M peptide in complex with human H3K9 methyltransferase G9a and SAM, which reveales that the methionine side chain had enhanced van der Waals interactions with G9a...
  60. Nguyen K, Das B, Dobrowolski C, Karn J. Multiple Histone Lysine Methyltransferases Are Required for the Establishment and Maintenance of HIV-1 Latency. MBio. 2017;8: pubmed publisher
    ..immunoprecipitation experiments, that both PRC2 and euchromatic histone-lysine N-methyltransferase 2 (EHMT2), the G9a H3K9me2-3 methyltransferase, are highly enriched at the proviral 5' long terminal repeat (LTR) and ..
  61. Montes De Oca R, Andreassen P, Wilson K. Barrier-to-Autointegration Factor influences specific histone modifications. Nucleus. 2011;2:580-90 pubmed publisher
    ..BAF associated in vivo with SET/I2PP2A (protein phosphatase 2A inhibitor; blocks H3 dephosphorylation) and G9a (H3-K9 methyltransferase), but showed no detectable association with HDAC1 or HATs...
  62. Venneti S, Felicella M, Coyne T, Phillips J, Gorovets D, Huse J, et al. Histone 3 lysine 9 trimethylation is differentially associated with isocitrate dehydrogenase mutations in oligodendrogliomas and high-grade astrocytomas. J Neuropathol Exp Neurol. 2013;72:298-306 pubmed publisher
    ..Furthermore, H3K9me3 may define a subset of grade II oligodendrogliomas with better overall survival. Our results suggest variable roles for IDH mutations in the pathogenesis of oligodendrogliomas versus astrocytic tumors. ..
  63. Xiong Y, Li F, Babault N, Wu H, Dong A, Zeng H, et al. Structure-activity relationship studies of G9a-like protein (GLP) inhibitors. Bioorg Med Chem. 2017;25:4414-4423 pubmed publisher
    Given the high homology between the protein lysine methyltransferases G9a-like protein (GLP) and G9a, it has been challenging to develop potent and selective inhibitors for either enzyme...
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    b>G9a is a mammalian histone methyltransferase that contributes to the epigenetic silencing of tumor suppressor genes...
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    ..of H3K56 monomethylation (H3K56me1) in mammalian cells and find that the histone lysine methytransferase G9a/KMT1C is required for H3K56me1 both in vivo and in vitro...
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    ..facultative heterochromatin formation by directly interacting with the histone H3 lysine 9 methyltransferase G9a. We found that heterochromatin protein 1 (HP1) and G9a formed a complex at the interleukin-1beta promoter that is ..
  67. Yuan X, Feng W, Imhof A, Grummt I, Zhou Y. Activation of RNA polymerase I transcription by cockayne syndrome group B protein and histone methyltransferase G9a. Mol Cell. 2007;27:585-95 pubmed
    ..Here we show that a complex consisting of CSB, RNA polymerase I (Pol I), and histone methyltransferase G9a is present at active rRNA genes...
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    ..03] and t105413c [P-recessive = 0.05], EHMT1-g-9441a [P (2df) = 0.05] and g41451t (P-trend = 0.04), and EHMT2-S237S [P (2df) = 0.04]. The most significant result was for DNMT3b-c31721t (P-trend = 0...
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    ..The histone methyltransferases measured here could be potential future therapeutic targets for small molecule pharmacology. ..
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    ..The clinicopathological correlation of G9a expression was assessed in tumor specimens of ovarian cancer patients...
  71. Chen C, Goyal P, Karimi M, Abildgaard M, Kimura H, Lorincz M. H3S10ph broadly marks early-replicating domains in interphase ESCs and shows reciprocal antagonism with H3K9me2. Genome Res. 2017;: pubmed publisher
    ..transcription initiation of genes co-oriented with the replication fork in Ehmt1-/- and Ehmt2-/- ESCs, indicating that establishment of repressive chromatin on the leading strand following DNA ..
  72. Mayr C, Helm K, Jakab M, Ritter M, Shrestha R, Makaju R, et al. The histone methyltransferase G9a: a new therapeutic target in biliary tract cancer. Hum Pathol. 2018;72:117-126 pubmed publisher
    The histone methyltransferase G9a (EHMT2) is a key enzyme for dimethylation of lysine 9 at histone 3 (H3K9me2), a suppressive epigenetic mark. G9a is over-expressed in tumor cells and contributes to cancer aggressiveness...