Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2

鉴定组蛋白赖氨酸甲基转移酶 EZH2 的强效、选择性、细胞活性抑制剂

阅读：4

作者：Sharad K Verma, Xinrong Tian, Louis V LaFrance, Céline Duquenne, Dominic P Suarez, Kenneth A Newlander, Stuart P Romeril, Joelle L Burgess, Seth W Grant, James A Brackley, Alan P Graves, Daryl A Scherzer, Art Shu, Christine Thompson, Heidi M Ott, Glenn S Van Aller, Carl A Machutta, Elsie Diaz, Yong

期刊：

ACS Medicinal Chemistry Letters

影响因子：

3.500

时间：

2012

起止号：

2012 Oct 19;3(12):1091-6.

doi：

10.1021/ml3003346

研究方向：

细胞生物学、表观遗传

细胞类型：

其它细胞

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.

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