International Union of Basic and Clinical Pharmacology. CXXII. Applying an objective evaluation to the status of class A orphan G protein-coupled receptors

Read full text
Authors: S P H Alexander, Kirstie A. Bennett, Andrew W. Brown, Michelle Glass, David E. Gloriam, Julien Hanson, Paul A. Insel, Eamonn Kelly, Christopher J. Langmead, Kirill A. Martemyanov, Rick R. Neubig, Stefan Offermanns
+7 more Mette M. Rosenkilde, Gunnar Schulte, Nicola J. Smith, Huixian Wu, Elena Faccenda, Simon D Harding, Anthony P. Davenport
Cited by: 1
References: 453

Abstract

), GPR65 (protons), GPR68 (protons), GPR132 (9-hydroxyoctadecadienoic acid), GPR183 (7α,25-dihydroxycholesterol), MRGPRD (β-alanine), and MRGPRX1 (bovine adrenal medulla peptide 8-22). The issue of nomenclature for these 10 GPCRs will be considered by further subcommittees of the Nomenclature and Standards Committee of the International Union of Basic and Clinical Pharmacology. We hope this review will prompt further investigations into these members of the currently most widely clinically exploited protein superfamily. SIGNIFICANCE STATEMENT: The use of systematic, rational nomenclature for drug targets provides a framework to ensure consistent identification and rapid recognition. Given that G protein-coupled receptors have fundamental physiological roles and are widespread targets of drugs in current clinical use, we hope the target summary and deorphanization criteria provided here will prompt renewed efforts to investigate these orphan receptors as regulators of physiology and as opportunities for future therapeutic exploitation.

Fields of Study & Subjects

Receptor Mechanisms and Signaling Diabetes Treatment and Management Blood Coagulation and Thrombosis Mechanisms

Publication details

Journal / source
Pharmacological Reviews
Publisher
Elsevier BV
Volume
78
Issue
4
Pages
100141–100141
Publication date
8 May 2026
Language
EN