EZH2: biology, disease, and structure-based drug discovery
文献类型：期刊论文
| 作者 | Tan, Jin-zhi1; Yan, Yan1; Wang, Xiao-xi1; Jiang, Yi1 ; Xu, H. Eric1,2
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| 刊名 | ACTA PHARMACOLOGICA SINICA
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| 出版日期 | 2014-02 |
| 卷号 | 35期号:2页码:161-174 |
| 关键词 | EZH2 PRC2 transcriptional repression gene activation anticancer drug crystal structure SET domain methyltransferase inhibitor epigenetic therapy |
| ISSN号 | 1671-4083 |
| DOI | 10.1038/aps.2013.161 |
| 文献子类 | Review |
| 英文摘要 | EZH2 is the catalytic subunit of the polycomb repressive complex 2 (PRC2), which is a highly conserved histone methyltransferase that methylates lysine 27 of histone 3. Overexpression of EZH2 has been found in a wide range of cancers, including those of the prostate and breast. In this review, we address the current understanding of the oncogenic role of EZH2, including its PRC2-dependent transcriptional repression and PRC2-independent gene activation. We also discuss the connections between EZH2 and other silencing enzymes, such as DNA methyltransferase and histone deacetylase. We comprehensively address the architecture of the PRC2 complex and the crucial roles of each subunit. Finally, we summarize new progress in developing EZH2 inhibitors, which could be a new epigenetic therapy for cancers. |
| WOS关键词 | HISTONE METHYLTRANSFERASE ACTIVITY ; GROUP PROTEIN EZH2 ; H3 LYSINE-27 METHYLATION ; POLYCOMB GROUP-COMPLEXES ; SMALL-MOLECULE INHIBITOR ; NON-HODGKIN-LYMPHOMA ; B-CELL LYMPHOMAS ; PROSTATE-CANCER ; BREAST-CANCER ; PRODUCT SPECIFICITY |
| 资助项目 | Jay and Betty Van Andel Foundation[00000000] ; National Natural Science Foundation of China[NSFC 81123004] ; Ministry of Science and Technology (China)[2012CB910403] ; Ministry of Science and Technology (China)[2013CB910601] ; Amway (USA)[00000000] |
| WOS研究方向 | Chemistry ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| CSCD记录号 | CSCD:5040822 |
| WOS记录号 | WOS:000330581300001 |
| 出版者 | ACTA PHARMACOLOGICA SINICA |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277210]  |
| 专题 | 药物靶标结构与功能中心 |
| 通讯作者 | Tan, Jin-zhi |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, VARI SIMM Ctr, Ctr Struct & Funct Drug Targets,Key Lab Receptor, Shanghai 201203, Peoples R China; 2.Van Andel Res Inst, Ctr Struct Biol & Drug Discovery, Lab Struct Sci, Grand Rapids, MI 49503 USA |
| 推荐引用方式 GB/T 7714 | Tan, Jin-zhi,Yan, Yan,Wang, Xiao-xi,et al. EZH2: biology, disease, and structure-based drug discovery[J]. ACTA PHARMACOLOGICA SINICA,2014,35(2):161-174. |
| APA | Tan, Jin-zhi,Yan, Yan,Wang, Xiao-xi,Jiang, Yi,&Xu, H. Eric.(2014).EZH2: biology, disease, and structure-based drug discovery.ACTA PHARMACOLOGICA SINICA,35(2),161-174. |
| MLA | Tan, Jin-zhi,et al."EZH2: biology, disease, and structure-based drug discovery".ACTA PHARMACOLOGICA SINICA 35.2(2014):161-174. |
入库方式： OAI收割
来源：上海药物研究所
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