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
收藏
页码：874 / 878
页数：5
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