Structure of the PRC2 complex and application to drug discovery
文献类型：期刊论文
| 作者 | Shi, Yi1 ; Wang, Xiao-xi1; Zhuang, You-wen1; Jiang, Yi1; Melcher, Karsten2; Xu, H. Eric1,2
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| 刊名 | ACTA PHARMACOLOGICA SINICA
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| 出版日期 | 2017-07 |
| 卷号 | 38期号:7页码:963-976 |
| 关键词 | PRC2 histone methyltransferase H3K27me3 nucleosome structure drug discovery |
| ISSN号 | 1671-4083 |
| DOI | 10.1038/aps.2017.7 |
| 文献子类 | Review |
| 英文摘要 | 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. |
| WOS关键词 | HISTONE METHYLTRANSFERASE ACTIVITY ; EMBRYONIC STEM-CELLS ; POLYCOMB GROUP PROTEINS ; NONCODING RNAS ; TARGETING EZH2 ; LYSINE METHYLTRANSFERASES ; DEVELOPMENTAL REGULATORS ; DROSOPHILA-MELANOGASTER ; H3K27 TRIMETHYLATION ; SELECTIVE-INHIBITION |
| 资助项目 | Ministry of Science and Technology of China[2012CB910403] ; Ministry of Science and Technology of China[2013CB910601] ; Chinese Academy of Sciences[XDB08020303] ; Outstanding Young Scientist Foundation, Chinese Academy of Sciences[00000000] ; Youth Innovation Promotion Association, Chinese Academy of Sciences[00000000] ; Jay and Betty Van Andel Foundation, Amway (USA)[00000000] |
| WOS研究方向 | Chemistry ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| CSCD记录号 | CSCD:6012583 |
| WOS记录号 | WOS:000404918600001 |
| 出版者 | ACTA PHARMACOLOGICA SINICA |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/272584]  |
| 专题 | 药物靶标结构与功能中心 |
| 通讯作者 | Shi, Yi; Xu, H. Eric |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, Ctr Struct & Funct Drug Targets, VARI SIMM Ctr,Key Lab Receptor Res, Shanghai 201203, Peoples R China; 2.Van Andel Res Inst, Lab Struct Sci, Grand Rapids, MI 49503 USA |
| 推荐引用方式 GB/T 7714 | Shi, Yi,Wang, Xiao-xi,Zhuang, You-wen,et al. Structure of the PRC2 complex and application to drug discovery[J]. ACTA PHARMACOLOGICA SINICA,2017,38(7):963-976. |
| APA | Shi, Yi,Wang, Xiao-xi,Zhuang, You-wen,Jiang, Yi,Melcher, Karsten,&Xu, H. Eric.(2017).Structure of the PRC2 complex and application to drug discovery.ACTA PHARMACOLOGICA SINICA,38(7),963-976. |
| MLA | Shi, Yi,et al."Structure of the PRC2 complex and application to drug discovery".ACTA PHARMACOLOGICA SINICA 38.7(2017):963-976. |
入库方式： OAI收割
来源：上海药物研究所
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