High-throughput screening of antagonists for the orphan G-protein coupled receptor GPR139
文献类型：期刊论文
| 作者 | Wang, Jia1,2 ; Zhu, Lin-yun1,2; Liu, Qing1,2; Hentzer, Morten3; Smith, Garrick Paul3; Wang, Ming-wei1,2
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| 刊名 | ACTA PHARMACOLOGICA SINICA
 |
| 出版日期 | 2015-07 |
| 卷号 | 36期号:7页码:874-878 |
| 关键词 | orphan G-protein coupled receptor GPR139 high-throughput screening calcium mobilization assay antagonist |
| ISSN号 | 1671-4083 |
| DOI | 10.1038/aps.2015.12 |
| 文献子类 | Article |
| 英文摘要 | Aim: To discover antagonists of the orphan G-protein coupled receptor GPR139 through high-throughput screening of a collection of diverse small molecules. Methods: Calcium mobilization assays were used to identify initial hits and for subsequent confirmation studies. Results: Five small molecule antagonists, representing 4 different scaffolds, were identified following high-throughput screening of 16 000 synthetic compounds. Conclusion: The findings provide important tools for further study of this orphan G-protein coupled receptor. |
| WOS关键词 | DISCOVERY |
| 资助项目 | National Health and Family Planning Commission of China[2012ZX09304-011] ; National Health and Family Planning Commission of China[2013ZX09401003-005] ; National Health and Family Planning Commission of China[2013ZX09507001] ; National Health and Family Planning Commission of China[2013ZX09507-002] ; Shanghai Science and Technology Development Fund[13DZ2290300] ; H Lundbeck A/S Denmark[00000000] ; Thousand Talents Program in China[00000000] |
| WOS研究方向 | Chemistry ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| CSCD记录号 | CSCD:5474158 |
| WOS记录号 | WOS:000357477600012 |
| 出版者 | ACTA PHARMACOLOGICA SINICA |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/276480]  |
| 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, Natl Ctr Drug Screening, Shanghai 201203, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, CAS Key Lab Receptor Res, Shanghai 201203, Peoples R China; 3.H Lundbeck & Co AS, Neurosci Drug Discovery, DK-2500 Copenhagen, Denmark |
| 推荐引用方式 GB/T 7714 | Wang, Jia,Zhu, Lin-yun,Liu, Qing,et al. High-throughput screening of antagonists for the orphan G-protein coupled receptor GPR139[J]. ACTA PHARMACOLOGICA SINICA,2015,36(7):874-878. |
| APA | Wang, Jia,Zhu, Lin-yun,Liu, Qing,Hentzer, Morten,Smith, Garrick Paul,&Wang, Ming-wei.(2015).High-throughput screening of antagonists for the orphan G-protein coupled receptor GPR139.ACTA PHARMACOLOGICA SINICA,36(7),874-878. |
| MLA | Wang, Jia,et al."High-throughput screening of antagonists for the orphan G-protein coupled receptor GPR139".ACTA PHARMACOLOGICA SINICA 36.7(2015):874-878. |
入库方式： OAI收割
来源：上海药物研究所
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