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Deprecated: Implicit conversion from float 231.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 ACS+Med+Chem+Lett 2012 ; 3 (12): 1091-6 Nephropedia Template TP
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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.