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

H3K27me3 binding to the EED pocket of the Polycomb repressive complex 2 (PRC2) is required to activate PRC2. An allosteric small-molecule inhibitor of PRC2 was identified that binds to the EED pocket and blocks PRC2 methyltransferase activity 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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