| Literature DB >> 24900432 |
Sharad K Verma1, Xinrong Tian1, Louis V LaFrance1, Céline Duquenne1, Dominic P Suarez1, Kenneth A Newlander1, Stuart P Romeril1, Joelle L Burgess1, Seth W Grant1, James A Brackley1, Alan P Graves1, Daryl A Scherzer1, Art Shu1, Christine Thompson1, Heidi M Ott1, Glenn S Van Aller1, Carl A Machutta1, Elsie Diaz1, Yong Jiang1, Neil W Johnson1, Steven D Knight1, Ryan G Kruger1, Michael T McCabe1, Dashyant Dhanak1, Peter J Tummino1, Caretha L Creasy1, William H Miller1.
Abstract
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.Entities:
Keywords: EZH2; Epigenetics; H3K27me3; PRC2; SAM-competitive inhibitor; methyltransferase
Year: 2012 PMID： 24900432 PMCID： PMC4025676 DOI： 10.1021/ml3003346
Source DB: PubMed Journal: ACS Med Chem Lett ISSN： 1948-5875 Impact factor: 4.345