Article
Polycomb repressive complex 2 structure with inhibitor reveals a mechanism of activation and drug resistance.
Nature communications - 28 Apr 2016
Brooun Alexei, Gajiwala Ketan S, Deng Ya-Li, Liu Wei, Bolaños Ben, Bingham Patrick, He You-Ai, Diehl Wade, Grable Nicole, Kung Pei-Pei, Sutton Scott, Maegley Karen A, Yu Xiu, Stewart Al E
Abstract excerpt
Polycomb repressive complex 2 (PRC2) mediates gene silencing through chromatin reorganization by methylation of histone H3 lysine 27 (H3K27). Overexpression of the complex and point mutations in the individual subunits of PRC2 have been shown to contribute to tumorigenesis. Several inhibitors of the PRC2 activity have shown efficacy in EZH2-mutated lymphomas and are currently in clinical development, although the...
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