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学科主题: 生命有机化学
题名: High-throughput screening of novel antagonists on melanin-concentrating hormone receptor-1
其他题名: High-throughput screening of novel antagonists on melanin-concentrating hormone receptor-1
作者: Xu X(徐信) ; Xu XY(徐小燕) ; Chen YF(陈耀峰) ; Sun J(孙杰)
通讯作者: 陈耀峰
刊名: Acta Pharmacol. Sin.
发表日期: 2008
卷: 29, 期:6, 页:752-758
收录类别: SCI
部门归属: 上海药物所; 法国Les Labs Servier; 上海有机所; 昆明植物所
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, [H-3]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-[S-35]thio) triphosphate ([S-35]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 [S-35]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.
语种: 英语
相关网址: 查看原文
WOS记录号: WOS:000256441900015
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内容类型: 期刊论文
URI标识: http://ir.sioc.ac.cn/handle/331003/21427
Appears in Collections:金属有机化学国家重点实验室_期刊论文

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Recommended Citation:
Xu X,Xu XY,Chen YF,et al. High-throughput screening of novel antagonists on melanin-concentrating hormone receptor-1[J]. Acta Pharmacol. Sin.,2008,29(6):752-758.
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