Identification of potent, selective, cell-active inhibitors of the histone lysine methyltransferase EZH2
SK Verma, X Tian, LV LaFrance… - ACS medicinal …, 2012 - ACS Publications
SK Verma, X Tian, LV LaFrance, C Duquenne, DP Suarez, KA Newlander, SP Romeril…
ACS medicinal chemistry letters, 2012•ACS PublicationsThe 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.
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.
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.
ACS Publications