High-throughput screening assay for new ligands at human melatonin receptors
文献类型：期刊论文
| 作者 | Yan, Jian-hua1,3; Su, Hao-ran1,3; Boutin, Jean A.2; Renard, M. Pierre2; Wang, Ming-wei1,3
|
| 刊名 | ACTA PHARMACOLOGICA SINICA
 |
| 出版日期 | 2008-12 |
| 卷号 | 29期号:12页码:1515-1521 |
| 关键词 | melatonin receptor selectivity agonist antagonist |
| ISSN号 | 1671-4083 |
| DOI | 10.1111/j.1745-7254.2008.00903.x |
| 文献子类 | Article |
| 英文摘要 | Aim: Melatonin (MT) is a neurohormone produced and secreted primarily by the pineal gland in a circadian manner, and mainly acts through 2 receptor subtypes: MT1 and MT2 in humans. The diversity in their tissue distribution is in favor of different functions for each receptor subtype. Selective modulators are therefore required to determine the physiological roles of these melatonin receptor subtypes and their implications in pathological processes. Methods: A homogenous MT1/MT2 receptor binding assay was established for high-throughput screening of new ligands at the hMT(1) and/or hMT(2) receptors. The functional properties (agonists or antagonists) were assessed by a conventional guanosine-5' [gamma-S-35] triphosphate (GTP-gamma S) assay. Results: Three hMT(1) receptor-selective small molecule antagonists and 1 hMT(2) receptor-selective small molecule antagonist with novel structural features were identified following a high-throughput screening campaign of 48 240 synthetic and natural compounds. Conclusion: The findings may assist in the expansion of chemical probes to these 2 receptor subtypes. |
| WOS关键词 | BINDING ; MT2 ; SUBTYPE ; MEL(1A) ; RETINA ; DISORDERS ; CLONING ; PINEAL ; BRAIN |
| 资助项目 | Shanghai Municipality Science and Technology Development Fund[06DZ22907] ; Shanghai Municipality Science and Technology Development Fund[07DZ22920] ; Ministry of Science and Technology[2004CB518902] ; Servier Beijing Pharmaceutical Research and Development[00000000] |
| WOS研究方向 | Chemistry ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| CSCD记录号 | CSCD:3430177 |
| WOS记录号 | WOS:000261710300015 |
| 出版者 | ACTA PHARMACOLOGICA SINICA |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/279412]  |
| 专题 | 国家新药筛选中心 中科院受体结构与功能重点实验室 新药研究国家重点实验室 |
| 通讯作者 | Wang, Ming-wei |
| 作者单位 | 1.Chinese Acad Sci, State Key Lab Drug Res, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China; 2.Les Labs Servier, F-92200 Neuilly Sur Seine, France 3.Chinese Acad Sci, Natl Ctr Drug Screening, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Yan, Jian-hua,Su, Hao-ran,Boutin, Jean A.,et al. High-throughput screening assay for new ligands at human melatonin receptors[J]. ACTA PHARMACOLOGICA SINICA,2008,29(12):1515-1521. |
| APA | Yan, Jian-hua,Su, Hao-ran,Boutin, Jean A.,Renard, M. Pierre,&Wang, Ming-wei.(2008).High-throughput screening assay for new ligands at human melatonin receptors.ACTA PHARMACOLOGICA SINICA,29(12),1515-1521. |
| MLA | Yan, Jian-hua,et al."High-throughput screening assay for new ligands at human melatonin receptors".ACTA PHARMACOLOGICA SINICA 29.12(2008):1515-1521. |
入库方式： OAI收割
来源：上海药物研究所
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