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Identification of (R)-N-((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide (CPI-1205), a Potent and Selective Inhibitor of Histone Methyltransferase EZH2, Suitable for Phase I Clinical Trials for B-Cell Lymphomas.
Vaswani RG, Gehling VS, Dakin LA, Cook AS, Nasveschuk CG, Duplessis M, Iyer P, Balasubramanian S, Zhao F, Good AC, Campbell R, Lee C, Cantone N, Cummings RT, Normant E, Bellon SF, Albrecht BK, Harmange JC, Trojer P, Audia JE, Zhang Y, Justin N, Chen S, Wilson JR, Gamblin SJ. Vaswani RG, et al. Among authors: gamblin sj. J Med Chem. 2016 Nov 10;59(21):9928-9941. doi: 10.1021/acs.jmedchem.6b01315. Epub 2016 Oct 28. J Med Chem. 2016. PMID: 27739677 Free PMC article.
Evolving Catalytic Properties of the MLL Family SET Domain.
Zhang Y, Mittal A, Reid J, Reich S, Gamblin SJ, Wilson JR. Zhang Y, et al. Among authors: gamblin sj. Structure. 2015 Oct 6;23(10):1921-1933. doi: 10.1016/j.str.2015.07.018. Epub 2015 Aug 27. Structure. 2015. PMID: 26320581 Free PMC article.
Role of the polycomb protein EED in the propagation of repressive histone marks.
Margueron R, Justin N, Ohno K, Sharpe ML, Son J, Drury WJ 3rd, Voigt P, Martin SR, Taylor WR, De Marco V, Pirrotta V, Reinberg D, Gamblin SJ. Margueron R, et al. Among authors: gamblin sj. Nature. 2009 Oct 8;461(7265):762-7. doi: 10.1038/nature08398. Epub 2009 Sep 20. Nature. 2009. PMID: 19767730 Free PMC article.
G-tract RNA removes Polycomb repressive complex 2 from genes.
Beltran M, Tavares M, Justin N, Khandelwal G, Ambrose J, Foster BM, Worlock KB, Tvardovskiy A, Kunzelmann S, Herrero J, Bartke T, Gamblin SJ, Wilson JR, Jenner RG. Beltran M, et al. Among authors: gamblin sj. Nat Struct Mol Biol. 2019 Oct;26(10):899-909. doi: 10.1038/s41594-019-0293-z. Epub 2019 Sep 23. Nat Struct Mol Biol. 2019. PMID: 31548724 Free PMC article.
109 results