Selective inhibition of Ezh2 by a small molecule inhibitor blocks tumor cells proliferation

Qi, Wei; Chan, Homan; Teng, Lin; Li, Ling; Chuai, Shannon; Zhang, Ruipeng; Zeng, Jue; Li, Min; Fan, Hong; Lin, Ying; Gu, Justin; Ardayfio, Ophelia; Zhang, Ji-Hu; Yan, Xiaoxia; Fang, Jialuo; Mi, Yuan; Zhang, Man; Zhou, Tao; Feng, Grace; Chen, Zijun; Li, Guobin; Yang, Teddy; Zhao, Kehao; Liu, Xianghui; Yu, Zhengtian; Lu, Chuang; Atadja, Peter; Li, En

doi:10.1073/pnas.1210371110

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Selective inhibition of Ezh2 by a small molecule inhibitor blocks tumor cells proliferation

Published in Proceedings of the National Academy of Sciences • Dec 10, 2012

Authors:

Wei Qi

Homan Chan

Lin Teng

Abstract

Ezh2 (Enhancer of zeste homolog 2) protein is the enzymatic component of the Polycomb repressive complex 2 (PRC2), which represses gene expression by methylating lysine 27 of histone H3 (H3K27) and regulates cell proliferation and differentiation during embryonic development. Recently, hot-spot muta...

Subject

EZH2

PRC2

Histone H3

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