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

共 50 条

[1] High-throughput screening of antagonists for the orphan G-protein coupled receptor GPR139
Jia Wang
Lin-yun Zhu
Qing Liu
Morten Hentzer
Garrick Paul Smith
Ming-wei Wang
Acta Pharmacologica Sinica, 2015, 36 : 874 - 878
[2] Identification of Surrogate Agonists and Antagonists for Orphan G-Protein-Coupled Receptor GPR139
Hu, Liaoyuan A.
Tang, Pauline M.
Eslahi, Nima K.
Zhou, Tian
Barbosa, Joseph
Liu, Qingyun
JOURNAL OF BIOMOLECULAR SCREENING, 2009, 14 (07) : 789 - 797
[3] Pharmacology and function of the orphan GPR139 G protein-coupled receptor
Vedel, Line
Nohr, Anne Cathrine
Gloriam, David E.
Brauner-Osborne, Hans
BASIC & CLINICAL PHARMACOLOGY & TOXICOLOGY, 2020, 126 : 35 - 46
[4] Molecular insights into ligand recognition and G protein coupling of the neuromodulatory orphan receptor GPR139
Yali Zhou
Henrik Daver
Boris Trapkov
Lijie Wu
Meng Wu
Kasper Harpsøe
Patrick R. Gentry
Kaiwen Liu
Marina Larionova
Junlin Liu
Na Chen
Hans Bräuner-Osborne
David E. Gloriam
Tian Hua
Zhi-Jie Liu
Cell Research, 2022, 32 : 210 - 213
[5] The role of orphan receptor GPR139 in neuropsychiatric behavior
Dao, Maria
Stoveken, Hannah M.
Cao, Yan
Martemyanov, Kirill A.
NEUROPSYCHOPHARMACOLOGY, 2022, 47 (04) : 902 - 913
[6] The role of orphan receptor GPR139 in neuropsychiatric behavior
Maria Dao
Hannah M. Stoveken
Yan Cao
Kirill A. Martemyanov
Neuropsychopharmacology, 2022, 47 : 902 - 913
[7] Pharmacological characterization of novel small molecule agonists and antagonists for the orphan receptor GPR139
Pallareti, Lisa
Rath, Tine F.
Trapkov, Boris
Tsonkov, Tsonko
Nielsen, Anders Thorup
Harpsoe, Kasper
Gentry, Patrick R.
Brauner-Osborne, Hans
Gloriam, David E.
Foster, Simon R.
EUROPEAN JOURNAL OF PHARMACOLOGY, 2023, 943
[8] Molecular insights into ligand recognition and G protein coupling of the neuromodulatory orphan receptor GPR139
Zhou, Yali
Daver, Henrik
Trapkov, Boris
Wu, Lijie
Wu, Meng
Harpsoe, Kasper
Gentry, Patrick R.
Liu, Kaiwen
Larionova, Marina
Liu, Junlin
Chen, Na
Brauner-Osborne, Hans
Gloriam, David E.
Hua, Tian
Liu, Zhi-Jie
CELL RESEARCH, 2022, 32 (02) : 210 - 213
[9] Novel Agonist Bioisosteres and Common Structure-Activity Relationships for The Orphan G Protein-Coupled Receptor GPR139
Shehata, Mohamed A.
Nohr, Anne C.
Lissa, Delphine
Bisig, Christoph
Isberg, Vignir
Andersen, Kirsten B.
Harpsoe, Kasper
Bjorkling, Fredrik
Brauner-Osborne, Hans
Gloriam, David E.
SCIENTIFIC REPORTS, 2016, 6
[10] Novel Agonist Bioisosteres and Common Structure-Activity Relationships for The Orphan G Protein-Coupled Receptor GPR139
Mohamed A. Shehata
Anne C. Nøhr
Delphine Lissa
Christoph Bisig
Vignir Isberg
Kirsten B. Andersen
Kasper Harpsøe
Fredrik Björkling
Hans Bräuner-Osborne
David E. Gloriam
Scientific Reports, 6

← 1 2 3 4 5 →