An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED

NATURE CHEMICAL BIOLOGY（2017）

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摘要

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.

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关键词

X-ray crystallography,Histone post-translational modifications,Small molecules,Cancer therapy

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