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10.1021/ml3003346

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C4025676!4025676!24900432
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suck abstract from ncbi


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pmid24900432      ACS+Med+Chem+Lett 2012 ; 3 (12): 1091-6
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  • Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2 #MMPMID24900432
  • Verma SK; Tian X; LaFrance L; Duquenne C; Suarez DP; Newlander KA; Romeril SP; Burgess JL; Grant SW; Brackley J; Graves AP; Scherzer DA; Shu A; Thompson C; Ott HM; Aller GSV; Machutta CA; Diaz E; Jiang Y; Johnson N; Knight SD; Kruger RG; McCabe MT; Dhanak D; Tummino P; Creasy CL; Miller WH
  • ACS Med Chem Lett 2012[Dec]; 3 (12): 1091-6 PMID24900432show ga
  • The histone H3-lysine 27 (H3K27) methyltransferase EZH2 plays a critical role in regulating gene expression, and its aberrant activity is linked to the onset and progression of cancer. As part of a drug discovery program targeting EZH2, we have identified highly potent, selective, SAM-competitive, and cell-active EZH2 inhibitors, including GSK926 (3) and GSK343 (6). These compounds are small molecule chemical tools that would be useful to further explore the biology of EZH2.
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