High-throughput screening of antagonists for the orphan G-protein coupled receptor GPR139

被引：23

作者：

Wang, Jia ^{[1
,2
]}

Zhu, Lin-yun ^{[1
,2
]}

Liu, Qing ^{[1
,2
]}

Hentzer, Morten ^{[3
]}

Smith, Garrick Paul ^{[3
]}

Wang, Ming-wei ^{[1
,2
]}

机构：

[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

来源：

ACTA PHARMACOLOGICA SINICA | 2015年 / 36卷 / 07期

关键词：

orphan G-protein coupled receptor; GPR139; high-throughput screening; calcium mobilization assay; antagonist; DISCOVERY;

D O I：

10.1038/aps.2015.12

中图分类号：

O6 [化学];

学科分类号：

0703 ;

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.

引用

页码：874 / 878

页数：5

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