The histone H3-
lysine 27 (H3K27) methy
ltransferase EZH2 p
lays a critica
l ro
le in regu
lating 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 high
ly potent, se
lective, SAM-competitive, and ce
ll-active EZH2 inhibitors, inc
luding GSK926 (
3) and GSK343 (
6). These compounds are sma
ll mo
lecu
le chemica
l too
ls that
wou
ld be usefu
l to further exp
lore the bio
logy of EZH2.
Keywords:
Epigenetics; EZH2; H3K27me3; ltransferase&qsSearchArea=searchText">methyltransferase; PRC2; SAM-competitive inhibitor