Alternative drug discovery approaches for orphan GPCRs

Drug Discovery Today
Angélique Levoye, Ralf Jockers

Abstract

G protein-coupled receptors (GPCRs) are well-known drug targets. However, a question mark remains for the more than 100 orphan GPCRs as current deorphanisation strategies failed to identify specific ligands for these receptors. Recent advances have shown that orphan GPCRs may have important functions that are ligand-independent. Orphan GPCRs can modulate the function of well-defined drug targets such as GPCRs with identified ligands and neurotransmitter transporters though physical association with those molecules. Thus, compounds that bind to orphan GPCRs and allosterically regulate the function of the interacting partner or even disrupt the interaction with the latter could become new drugs.

Citations

Oct 17, 2009·Journal de la Société de biologie·Bernard Scatton
Aug 6, 2016·Molecular Informatics·Shao-Xing DaiJing-Fei Huang
May 30, 2009·Drug Discovery Today·Bhushan Patwardhan, Raghunath Anant Mashelkar
Jan 30, 2008·Biotechnology Journal·Johan BacartCyril Couturier
Sep 19, 2014·British Journal of Pharmacology·Raise AhmadRalf Jockers
May 22, 2008·British Journal of Pharmacology·R JockersP Delagrange
Apr 13, 2018·Frontiers in Molecular Neuroscience·Wu ZhengJiang-Fan Chen
May 18, 2018·Nature Communications·Maurizio MorriHarald Janovjak

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