An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED

Wei Qi,Kehao Zhao,Justin Gu,Ying Huang,Youzhen Wang,Hailong Zhang,Man Zhang,Ji-Hu Zhang,Zhengtian Yu,Ling Li,Lin Teng,Shannon Chuai,Chao Zhang,Mengxi Zhao,HoMan Chan,Zijun Chen,Douglas D. Fang,Qi Fei,Lijian Feng,Yuan Gao,Hui Ge,X Ge,Guobin Li,Andreas Lingel,Ying Lin,Yueqin Liu,Fangjun Luo,Minlong Shi,Long Wang,Zhaofu Wang,Yenyen Yu,Jue Zeng,Chenhui Zeng,Lijun Zhang,Q. Zhang,Shaolian Zhou,Counde Oyang,Peter Atadja,En Li

An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED

2017

Wei Qi
Kehao Zhao
Justin Gu
Ying Huang
Youzhen Wang
Hailong Zhang
Man Zhang
Ji-Hu Zhang
Zhengtian Yu
Ling Li
Lin Teng
Shannon Chuai
Chao Zhang
Mengxi Zhao
HoMan Chan
Zijun Chen
Douglas D. Fang
Qi Fei
Lijian Feng
Yuan Gao
Hui Ge
X Ge
Guobin Li
Andreas Lingel
Ying Lin
Yueqin Liu
Fangjun Luo
Minlong Shi
Long Wang
Zhaofu Wang
Yenyen Yu
Jue Zeng
Chenhui Zeng
Lijun Zhang
Q. Zhang
Shaolian Zhou
Counde Oyang
Peter Atadja
En Li

H3K27me3 binding to the EED pocket of the Polycomb repressive complex 2 ( PRC2) is required to activate PRC2. An allosteric small-moleculeinhibitor of PRC2was identified that binds to the EED pocket and blocks PRC2 methyltransferaseactivity in cells.

Keywords:

PRC2
Polycomb Repressive Complex 2
Small molecule
Biochemistry
Molecular biology
Biology
Methyltransferase
Allosteric regulation
Histone
Lysine
Binding site
Structure–activity relationship

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