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题名: High-throughput screening of novel antagonists on melanin-concentrating hormone receptor-1
作者: Yan, Jian-hua1, 2; Li, Qun-yi1, 2; Boutin, Jean A.3; Renard, M. Pierre3; Ding, Yi-xiang4; null(郝小江)5; Zhao, Wei-min1, 2; Wang, Ming-wei1, 2
刊名: ACTA PHARMACOLOGICA SINICA
关键词: melanin-concentrating hormone ; melanin-concentrating hormone receptor-1 ; antagonist
英文摘要: Aim: To find new antagonists on human melanin-concentrating hormone recep-tor-1 (MCHR-1) through high-throughput screening (HTS) of a diverse compound library. Methods: MCHR-1, [(3)H]SNAP7941, and FlashBlue G-protein-coupled receptor beads were used to measure the receptor-binding activities of various compounds based on scintillation proximity assay (SPA) technology. The guanosine 5' (gamma-[(35)S]thio) triphosphate ([(35)S]GTP gamma S) binding assay was subsequently applied to functionally characterize the "hits" identified by the HTS campaign. Results: Of the 48 240 compounds screened with the SPA method, 12 hits were confirmed to possess MCHR-1 binding activities, 8 were functionally studied subsequently with the [(35)S]GTP gamma S binding assay, and only 1 compound (NC127816) displayed moderate human MCHR-1 binding affinity (K(i)=115.7 nmol/L) and relatively potent antagonism (K(B)=23.8 nmol/L). This compound shares a novel scaffold (1-ethoxy-2H-2-aza-1-phospha-naphthalene 1-oxide) with 3 other analogs in the group. Conclusion: Considering the marked difference in molecular shape and electrostatic status between NC127816 and the structures reported elsewhere, we anticipate that its derivatives may represent a new class of potent MCHR-1 modulators.
出版日期: 2008-06-01
卷号: 29, 期号:6, 页码:752-758
DOI标识: 10.1111/j.1745-7254.2008.00800.x
语种: 英语
ISSN号: 1671-4083
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.kib.ac.cn/handle/151853/2929
Appears in Collections:植物化学与西部植物资源持续利用国家重点实验室_期刊论文

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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, State Key Lab New Drug Res, Shanghai 201203, Peoples R China
3.Les Labs Servier, F-92200 Neuillly Sur Seine, France
4.Chinese Acad Sci, Shanghai Inst Organ Chem, Shanghai 200032, Peoples R China
5.Chinese Acad Sci, Kunming Inst Bot, Kunming 650204, Peoples R China

Recommended Citation:
Yan, JH; Li, QY; Boutin, JA; Renard, MP; Ding, YX; Hao, XJ; Zhao, WM; Wang, MW.High-throughput screening of novel antagonists on melanin-concentrating hormone receptor-1,ACTA PHARMACOLOGICA SINICA,2008,29(6):752-758
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