Polycomb repressive complex 2 structure with inhibitor reveals a mechanism of activation and drug resistance

@inproceedings{Brooun2016PolycombRC,
  title={Polycomb repressive complex 2 structure with inhibitor reveals a mechanism of activation and drug resistance},
  author={Alexei Brooun and Ketan Satish Gajiwala and Ya-Li Deng and Wei Ting Liu and Ben J Bola{\~n}os and Patrick Bingham and You-ai He and Wade Diehl and Nicole Grable and Pei-Pei Kung and Scott Channing Sutton and Karen A. Maegley and Xiu Xia Yu and Jamie Stewart},
  booktitle={Nature communications},
  year={2016}
}
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 molecular basis of inhibitor recognition remains unknown. Here we report the… CONTINUE READING
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