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Chromatin biology

Breaking into the PRC2 cage

Nature Chemical Biology volume 13, pages 345–346 (2017)Cite this article

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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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Authors and Affiliations

  1. Daniel Holoch & Raphaël Margueron are at the Department of Genetics and Developmental Biology, Institut Curie-PSL Research University, CNRS UMR3215, INSERM U934, Paris, France.,

    Daniel Holoch & Raphaël Margueron

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  1. Daniel Holoch
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  2. Raphaël Margueron
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Correspondence to Raphaël Margueron.

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The authors declare no competing financial interests.

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Holoch, D., Margueron, R. Breaking into the PRC2 cage. Nat Chem Biol 13, 345–346 (2017). https://doi.org/10.1038/nchembio.2313

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