The histone H3-lysine 27 (H3K27) methyltransferase EZH2 plays a critical role in regulating gene expression, and its aberrant acti
vity is linked to the onset and progression of cancer. As part of a drug disco
very program targeting EZH2, we ha
ve identified highly potent, selecti
ve, SAM-competiti
ve, and cell-acti
ve 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.
Keywords:
Epigenetics; EZH2; H3K27me3; methyltransferase; PRC2; ve+inhibitor&qsSearchArea=searchText">SAM-competitive inhibitor