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A small-molecule probe of the histone methyltransferase G9a induces cellular senescence in pancreatic adenocarcinoma.

Yuan Y, Wang Q, Paulk J, Kubicek S, Kemp MM, Adams DJ, Shamji AF, Wagner BK, Schreiber SL.

ACS Chem Biol. 2012 Jul 20;7(7):1152-7. doi: 10.1021/cb300139y. Epub 2012 Apr 30.


Gossypol and an HMT G9a inhibitor act in synergy to induce cell death in pancreatic cancer cells.

Yuan Y, Tang AJ, Castoreno AB, Kuo SY, Wang Q, Kuballa P, Xavier R, Shamji AF, Schreiber SL, Wagner BK.

Cell Death Dis. 2013 Jun 27;4:e690. doi: 10.1038/cddis.2013.191.


Depletion of G9a gene induces cell apoptosis in human gastric carcinoma.

Lin X, Huang Y, Zou Y, Chen X, Ma X.

Oncol Rep. 2016 May;35(5):3041-9. doi: 10.3892/or.2016.4692. Epub 2016 Mar 17.


Arsenic silences hepatic PDK4 expression through activation of histone H3K9 methylatransferase G9a.

Zhang X, Wu J, Choiniere J, Yang Z, Huang Y, Bennett J, Wang L.

Toxicol Appl Pharmacol. 2016 Aug 1;304:42-7. doi: 10.1016/j.taap.2016.05.015. Epub 2016 May 20.


Inhibition of H3K9 histone methyltransferase G9a attenuates renal fibrosis and retains klotho expression.

Irifuku T, Doi S, Sasaki K, Doi T, Nakashima A, Ueno T, Yamada K, Arihiro K, Kohno N, Masaki T.

Kidney Int. 2016 Jan;89(1):147-57. doi: 10.1038/ki.2015.291. Epub 2016 Jan 4.


Synthesis and biological evaluation of benzimidazole derivatives as the G9a Histone Methyltransferase inhibitors that induce autophagy and apoptosis of breast cancer cells.

Zhang J, Yao D, Jiang Y, Huang J, Yang S, Wang J.

Bioorg Chem. 2017 Jun;72:168-181. doi: 10.1016/j.bioorg.2017.04.005. Epub 2017 Apr 17.


G9a orchestrates PCL3 and KDM7A to promote histone H3K27 methylation.

Pan MR, Hsu MC, Chen LT, Hung WC.

Sci Rep. 2015 Dec 21;5:18709. doi: 10.1038/srep18709.


G9a - An Appealing Antineoplastic Target.

Chen WL, Sun HP, Li DD, Wang ZH, You QD, Guo XK.

Curr Cancer Drug Targets. 2017;17(6):555-568. doi: 10.2174/1568009616666160512145303. Review.


The histone methyltransferase G9a as a therapeutic target to override gemcitabine resistance in pancreatic cancer.

Pan MR, Hsu MC, Luo CW, Chen LT, Shan YS, Hung WC.

Oncotarget. 2016 Sep 20;7(38):61136-61151. doi: 10.18632/oncotarget.11256.


H3K9 histone methyltransferase G9a promotes lung cancer invasion and metastasis by silencing the cell adhesion molecule Ep-CAM.

Chen MW, Hua KT, Kao HJ, Chi CC, Wei LH, Johansson G, Shiah SG, Chen PS, Jeng YM, Cheng TY, Lai TC, Chang JS, Jan YH, Chien MH, Yang CJ, Huang MS, Hsiao M, Kuo ML.

Cancer Res. 2010 Oct 15;70(20):7830-40. doi: 10.1158/0008-5472.CAN-10-0833. Epub 2010 Oct 12.


Coordinated recruitment of histone methyltransferase G9a and other chromatin-modifying enzymes in SHP-mediated regulation of hepatic bile acid metabolism.

Fang S, Miao J, Xiang L, Ponugoti B, Treuter E, Kemper JK.

Mol Cell Biol. 2007 Feb;27(4):1407-24. Epub 2006 Dec 4.


The histone H3 methyltransferase G9A epigenetically activates the serine-glycine synthesis pathway to sustain cancer cell survival and proliferation.

Ding J, Li T, Wang X, Zhao E, Choi JH, Yang L, Zha Y, Dong Z, Huang S, Asara JM, Cui H, Ding HF.

Cell Metab. 2013 Dec 3;18(6):896-907. doi: 10.1016/j.cmet.2013.11.004.


Involvement of histone H3 lysine 9 (H3K9) methyltransferase G9a in the maintenance of HIV-1 latency and its reactivation by BIX01294.

Imai K, Togami H, Okamoto T.

J Biol Chem. 2010 May 28;285(22):16538-45. doi: 10.1074/jbc.M110.103531. Epub 2010 Mar 24.


Histone-lysine methyltransferase EHMT2 is involved in proliferation, apoptosis, cell invasion, and DNA methylation of human neuroblastoma cells.

Lu Z, Tian Y, Salwen HR, Chlenski A, Godley LA, Raj JU, Yang Q.

Anticancer Drugs. 2013 Jun;24(5):484-93. doi: 10.1097/CAD.0b013e32835ffdbb.


Post-translational modifications of histones H3 and H4 associated with the histone methyltransferases Suv39h1 and G9a.

Robin P, Fritsch L, Philipot O, Svinarchuk F, Ait-Si-Ali S.

Genome Biol. 2007;8(12):R270.


Inhibition of H3K9 methyltransferase G9a induces autophagy and apoptosis in oral squamous cell carcinoma.

Ren A, Qiu Y, Cui H, Fu G.

Biochem Biophys Res Commun. 2015 Mar 27;459(1):10-7. doi: 10.1016/j.bbrc.2015.01.068. Epub 2015 Jan 26.


Properly substituted analogues of BIX-01294 lose inhibition of G9a histone methyltransferase and gain selective anti-DNA methyltransferase 3A activity.

Rotili D, Tarantino D, Marrocco B, Gros C, Masson V, Poughon V, Ausseil F, Chang Y, Labella D, Cosconati S, Di Maro S, Novellino E, Schnekenburger M, Grandjenette C, Bouvy C, Diederich M, Cheng X, Arimondo PB, Mai A.

PLoS One. 2014 May 8;9(5):e96941. doi: 10.1371/journal.pone.0096941. eCollection 2014.


The Histone Methyltransferase Inhibitor A-366 Uncovers a Role for G9a/GLP in the Epigenetics of Leukemia.

Pappano WN, Guo J, He Y, Ferguson D, Jagadeeswaran S, Osterling DJ, Gao W, Spence JK, Pliushchev M, Sweis RF, Buchanan FG, Michaelides MR, Shoemaker AR, Tse C, Chiang GG.

PLoS One. 2015 Jul 6;10(7):e0131716. doi: 10.1371/journal.pone.0131716. eCollection 2015.


A subset of the histone H3 lysine 9 methyltransferases Suv39h1, G9a, GLP, and SETDB1 participate in a multimeric complex.

Fritsch L, Robin P, Mathieu JR, Souidi M, Hinaux H, Rougeulle C, Harel-Bellan A, Ameyar-Zazoua M, Ait-Si-Ali S.

Mol Cell. 2010 Jan 15;37(1):46-56. doi: 10.1016/j.molcel.2009.12.017.

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