Chemerin Receptor 2 Antibodies

Chemerin receptor 2, encoded by GPR1, is a class A G protein-coupled receptor activated by the adipokine chemerin. The chemerin-derived C-terminal nonapeptide C9 also activates GPR1 and is used as an experimental agonist. In recombinant systems, human GPR1 recruits β-arrestins robustly but shows relatively weak G protein signaling. Chemerin stimulation promotes β-arrestin recruitment and receptor internalization, and agonist-independent association with β-arrestin has also been observed. GPR1 can internalize bound chemerin in cell-based assays, suggesting a role in regulating local chemerin availability. GPR1 expression has been reported in adipose tissue and skeletal muscle, and studies in knockout mice suggest that it contributes to glucose homeostasis under high-fat feeding. Its physiological role in humans remains incompletely understood. No GPR1-selective ligand has been reported to enter clinical trials or receive approval for therapeutic use. The Chemerin2 receptor is regulated by phosphorylation of carboxyl-terminal serine331/serine333 (pS331/pS333-CMKLR2), threonine335/serine337 (pT335/pS337-CMKLR2) and serine343/threonine345 (pS343/pT345-CMKLR2). This nomenclature refers to the human CMKLR2. This phosphorylation motif is highly conserved across species and nearly identical in mice, rats and humans. For more information on CMKLR2 pharmacology please refer to the IUPHAR database. For further reading refer to:

Kennedy AJ, Davenport AP. International Union of Basic and Clinical Pharmacology CIII: Chemerin Receptors CMKLR1 (Chemerin1) and GPR1 (Chemerin2) Nomenclature, Pharmacology, and Function. Pharmacol Rev. 2018 Jan;70(1):174-196. doi: 10.1124/pr.116.013177. Epub 2017 Dec 26. PMID: 29279348

Davenport AP, Monaghan AE. Chemerin receptors (version 2019.3) in the IUPHAR/BPS Guide to Pharmacology Database. IUPHAR/BPS Guide to Pharmacology CITE. 2019; 2019(3). Available from: https://doi.org/10.2218/gtopdb/F338/2021.3.