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Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2

2012; American Chemical Society; Volume: 3; Issue: 12 Linguagem: Inglês

10.1021/ml3003346

1948-5875

Sharad K. Verma, Xinrong Tian, Louis V. LaFrance, Céline Duquenne, Dominic Suarez, Kenneth A. Newlander, Stuart P. Romeril, Joelle L. Burgess, Seth W. Grant, James Brackley, Alan P. Graves, D. Scherzer, Art Shu, Christine Thompson, Heidi M. Ott, Glenn S. Van Aller, Carl A. Machutta, Elsie Diaz, Yong Jiang, Neil W. Johnson, Steven D. Knight, Ryan G. Kruger, Michael T. McCabe, Dashyant Dhanak, Peter J. Tummino, Caretha L. Creasy, William H. Miller,

RNA modifications and cancer

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.