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Epigenetics

Stopping a chromatin enzyme

The first direct chemical inhibitor of a key histone-methylating enzyme provides a new tool to alter epigenetic states and genome expression profiles in normal and cancer cells.

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Figure 1: PRC2 subunit composition and modes of inhibition.

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Correspondence to Jeffrey A Simon.

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Note added in proof: The discovery of another selective SAM-competitive PRC2 inhibitor, structurally related to the one described by Knutson et al.1, has recently been reported12. Significantly, this related inhibitor is shown to have antitumor effects on EZH2 mutant xenografts in mice.

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Simon, J. Stopping a chromatin enzyme. Nat Chem Biol 8, 875–876 (2012). https://doi.org/10.1038/nchembio.1088

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