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Chromatin biology

Breaking into the PRC2 cage

New small-molecule inhibitors of the histone methyltransferase PRC2 interfere with the allosteric activation of enzymatic activity. These compounds are effective against PRC2-dependent tumors that are resistant to catalytic inhibitors and provide important new tools for altering chromatin regulation.

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Figure 1: PRC2 inhibitors target the product-driven stimulation of enzymatic activity.


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Correspondence to Raphaël Margueron.

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Holoch, D., Margueron, R. Breaking into the PRC2 cage. Nat Chem Biol 13, 345–346 (2017).

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