A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells

NATURE CHEMICAL BIOLOGY（2012）

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摘要

EZH2 is a protein methyltransferase component of the polycomb repressive complex 2 (PRC2) that installs the H3K27me3 chromatin mark. EPZ005687 inhibits EZH2 function and H3K27 trimethylation in cells and selectively kills lymphoma cells that require EZH2 for proliferation.

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nature chemical biology, science

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