1.
ACS Med Chem Lett
; 3(12): 1091-6, 2012 Dec 13.
Artigo
em Inglês
| MEDLINE
| ID: mdl-24900432
RESUMO
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.