2. Academic Validation
  3. Structure of the PRC2 complex and application to drug discovery

Structure of the PRC2 complex and application to drug discovery

  • Acta Pharmacol Sin. 2017 Jul;38(7):963-976. doi: 10.1038/aps.2017.7.
Yi Shi 1,  Xiao-Xi Wang 1,  You-Wen Zhuang 1,  Yi Jiang 1,  Karsten Melcher 2,  H Eric Xu 1 2
Affiliations

Affiliations

  • 1 Key Laboratory of Receptor Research, VARI-SIMM Center, Center for Structure and Function of Drug Targets, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
  • 2 Laboratory of Structural Sciences, Van Andel Research Institute, Grand Rapids, MI 49503, USA.
PMID: 28414199 DOI: 10.1038/aps.2017.7
Abstract

The polycomb repressive complexes 2 (PRC2) complex catalyzes tri-methylation of histone H3 lysine 27 (H3K27), a repressive chromatin marker associated with gene silencing. Overexpression and mutations of PRC2 are found in a wide variety of cancers, making the catalytic activity of PRC2 an important target of Cancer therapy. This review highlights recent structural breakthroughs of the human PRC2 complex bound to the H3K27 peptide and a small molecule inhibitor, which provide critically needed insight into PRC2-targeted drug discovery.

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