Histone lysine methyltransferases as anti-cancer targets for drug discovery
文献类型：期刊论文
| 作者 | Liu, Qing1,2,3; Wang, Ming-wei1,2,3
|
| 刊名 | ACTA PHARMACOLOGICA SINICA
 |
| 出版日期 | 2016-10 |
| 卷号 | 37期号:10页码:1273-1280 |
| 关键词 | histone methyltransferases adenosylmethionine small molecule inhibitors anti-cancer drugs epigenetic modification drug discovery |
| ISSN号 | 1671-4083 |
| DOI | 10.1038/aps.2016.64 |
| 文献子类 | Review |
| 英文摘要 | Post-translational epigenetic modification of histones is controlled by a number of histone-modifying enzymes. Such modification regulates the accessibility of DNA and the subsequent expression or silencing of a gene. Human histone methyltransferases (HMTs) constitute a large family that includes histone lysine methyltransferases (HKMTs) and histone/protein arginine methyltransferases (PRMTs). There is increasing evidence showing a correlation between HKMTs and cancer pathogenesis. Here, we present an overview of representative HKMTs, including their biological and biochemical properties as well as the profiles of small molecule inhibitors for a comprehensive understanding of HKMTs in drug discovery. |
| WOS关键词 | SMALL-MOLECULE INHIBITOR ; SELECTIVE INHIBITOR ; MODIFYING ENZYMES ; STRUCTURAL BASIS ; SEQUENCE MOTIFS ; EZH2 ; METHYLATION ; SMYD2 ; G9A ; DOT1L |
| 资助项目 | National Health and Family Planning Commission[2012ZX09304-011] ; National Health and Family Planning Commission[2013ZX09401003-005] ; National Health and Family Planning Commission[2013ZX09507001] ; National Health and Family Planning Commission[2013ZX09507-002] ; National Health and Family Planning Commission[2014ZX09507002-001] ; National Natural Science Foundation of China[21302202] ; Shanghai Science and Technology Development Fund[15DZ2291600] ; Thousand Talents Program in China[00000000] |
| WOS研究方向 | Chemistry ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| CSCD记录号 | CSCD:5820837 |
| WOS记录号 | WOS:000385634300001 |
| 出版者 | ACTA PHARMACOLOGICA SINICA |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/275875]  |
| 专题 | 国家新药筛选中心 |
| 通讯作者 | Wang, Ming-wei |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, CAS Key Lab Receptor Res, Shanghai 201203, Peoples R China; 2.Natl Ctr Drug Screening, Shanghai 201203, Peoples R China; 3.Fudan Univ, Sch Pharm, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Liu, Qing,Wang, Ming-wei. Histone lysine methyltransferases as anti-cancer targets for drug discovery[J]. ACTA PHARMACOLOGICA SINICA,2016,37(10):1273-1280. |
| APA | Liu, Qing,&Wang, Ming-wei.(2016).Histone lysine methyltransferases as anti-cancer targets for drug discovery.ACTA PHARMACOLOGICA SINICA,37(10),1273-1280. |
| MLA | Liu, Qing,et al."Histone lysine methyltransferases as anti-cancer targets for drug discovery".ACTA PHARMACOLOGICA SINICA 37.10(2016):1273-1280. |
入库方式： OAI收割
来源：上海药物研究所
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