Abstract
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.
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Acknowledgements
This work was partially supported by grants from the National Health and Family Planning Commission of China (2012ZX09304-011, 2013ZX09401003-005, 2013ZX09507001, and 2013ZX09507-002), the Shanghai Science and Technology Development Fund (13DZ2290300), H Lundbeck A/S Denmark and the Thousand Talents Program in China.
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Wang, J., Zhu, Ly., Liu, Q. et al. High-throughput screening of antagonists for the orphan G-protein coupled receptor GPR139. Acta Pharmacol Sin 36, 874–878 (2015). https://doi.org/10.1038/aps.2015.12
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DOI: https://doi.org/10.1038/aps.2015.12
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