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

Polycomb repressive complex 2 (PRC2) mediates gene silencing through chromatin reorganization by methylation of histone H3 lysine 27 (H3K27). Here, the authors present crystal structures of the inhibitor-bound wild-type and a mutant form of PRC2.

Bibliographic Details
Main Authors: Alexei Brooun, Ketan S. Gajiwala, Ya-Li Deng, Wei Liu, Ben Bolaños, Patrick Bingham, You-Ai He, Wade Diehl, Nicole Grable, Pei-Pei Kung, Scott Sutton, Karen A. Maegley, Xiu Yu, Al E. Stewart
Format: Article
Language:English
Published: Nature Portfolio 2016-04-01
Series:Nature Communications
Online Access:https://doi.org/10.1038/ncomms11384
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author Alexei Brooun
Ketan S. Gajiwala
Ya-Li Deng
Wei Liu
Ben Bolaños
Patrick Bingham
You-Ai He
Wade Diehl
Nicole Grable
Pei-Pei Kung
Scott Sutton
Karen A. Maegley
Xiu Yu
Al E. Stewart
author_facet Alexei Brooun
Ketan S. Gajiwala
Ya-Li Deng
Wei Liu
Ben Bolaños
Patrick Bingham
You-Ai He
Wade Diehl
Nicole Grable
Pei-Pei Kung
Scott Sutton
Karen A. Maegley
Xiu Yu
Al E. Stewart
author_sort Alexei Brooun
collection DOAJ
description Polycomb repressive complex 2 (PRC2) mediates gene silencing through chromatin reorganization by methylation of histone H3 lysine 27 (H3K27). Here, the authors present crystal structures of the inhibitor-bound wild-type and a mutant form of PRC2.
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spelling doaj.art-845df6d19e6c440e8657bbebe46e34a82022-12-21T19:26:35ZengNature PortfolioNature Communications2041-17232016-04-017111210.1038/ncomms11384Polycomb repressive complex 2 structure with inhibitor reveals a mechanism of activation and drug resistanceAlexei Brooun0Ketan S. Gajiwala1Ya-Li Deng2Wei Liu3Ben Bolaños4Patrick Bingham5You-Ai He6Wade Diehl7Nicole Grable8Pei-Pei Kung9Scott Sutton10Karen A. Maegley11Xiu Yu12Al E. Stewart13Worldwide Medicinal Chemistry, Worldwide Research and Development, Pfizer Inc.Worldwide Medicinal Chemistry, Worldwide Research and Development, Pfizer Inc.Worldwide Medicinal Chemistry, Worldwide Research and Development, Pfizer Inc.Worldwide Medicinal Chemistry, Worldwide Research and Development, Pfizer Inc.Worldwide Medicinal Chemistry, Worldwide Research and Development, Pfizer Inc.Oncology Research Unit, Worldwide Research and Development, Pfizer Inc.Worldwide Medicinal Chemistry, Worldwide Research and Development, Pfizer Inc.Worldwide Medicinal Chemistry, Worldwide Research and Development, Pfizer Inc.Worldwide Medicinal Chemistry, Worldwide Research and Development, Pfizer Inc.Worldwide Medicinal Chemistry, Worldwide Research and Development, Pfizer Inc.Worldwide Medicinal Chemistry, Worldwide Research and Development, Pfizer Inc.Oncology Research Unit, Worldwide Research and Development, Pfizer Inc.Worldwide Medicinal Chemistry, Worldwide Research and Development, Pfizer Inc.Worldwide Medicinal Chemistry, Worldwide Research and Development, Pfizer Inc.Polycomb repressive complex 2 (PRC2) mediates gene silencing through chromatin reorganization by methylation of histone H3 lysine 27 (H3K27). Here, the authors present crystal structures of the inhibitor-bound wild-type and a mutant form of PRC2.https://doi.org/10.1038/ncomms11384
spellingShingle Alexei Brooun
Ketan S. Gajiwala
Ya-Li Deng
Wei Liu
Ben Bolaños
Patrick Bingham
You-Ai He
Wade Diehl
Nicole Grable
Pei-Pei Kung
Scott Sutton
Karen A. Maegley
Xiu Yu
Al E. Stewart
Polycomb repressive complex 2 structure with inhibitor reveals a mechanism of activation and drug resistance
Nature Communications
title Polycomb repressive complex 2 structure with inhibitor reveals a mechanism of activation and drug resistance
title_full Polycomb repressive complex 2 structure with inhibitor reveals a mechanism of activation and drug resistance
title_fullStr Polycomb repressive complex 2 structure with inhibitor reveals a mechanism of activation and drug resistance
title_full_unstemmed Polycomb repressive complex 2 structure with inhibitor reveals a mechanism of activation and drug resistance
title_short Polycomb repressive complex 2 structure with inhibitor reveals a mechanism of activation and drug resistance
title_sort polycomb repressive complex 2 structure with inhibitor reveals a mechanism of activation and drug resistance
url https://doi.org/10.1038/ncomms11384
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