GPR132 Receptor Antibodies

G protein-coupled receptor 132 (GPR132, also known as G2A), encoded by GPR132, is a class A receptor implicated in immune responses to lipid and metabolic cues. The oxidized linoleic acid derivative 9-hydroxyoctadecadienoic acid (9-HODE) and N-palmitoylglycine can activate GPR132 in experimental systems, although their physiological relevance as endogenous agonists remains incompletely established. GPR132 can engage Gi-dependent pathways, and candidate lipid agonists can elicit intracellular calcium mobilization and β-arrestin recruitment in cell-based assays. The receptor is expressed in several leukocyte populations, including monocytes, macrophages, and lymphocytes. Experimental studies implicate GPR132 in the regulation of immune cell migration and macrophage activation. In mouse tumor models, macrophage GPR132 has been linked to responses to a lactate-rich microenvironment, although direct activation of the receptor by lactate remains unestablished. Different lipid agonists vary in their ability to recruit β-arrestin, and the mechanisms governing receptor desensitization and trafficking in native cells remain poorly characterized. The small molecule SB-583355 has been used as an experimental GPR132 antagonist, and no GPR132-selective drug has been reported to enter clinical trials or receive approval for therapeutic use. GPR132 is regulated by phosphorylation of carboxyl-terminal threonine339/serine341 (pT339/pS341-GPR132), threonine344/serine349 (pT344/pS349-GPR132) and threonine358/serine360 (pT344/pS360-GPR132). This nomenclature refers to the human GPR132 receptor. For more information on GPR132 pharmacology please refer to the IUPHAR database. For further reading refer to:

Alexander SP, Battey J, Benson HE, Benya RV, Bonner TI, Davenport AP, Dhanachandra Singh K, Eguchi S, Harmar A, Holliday N, Jensen RT, Karnik S, Kostenis E, Liew WC, Monaghan AE, Mpamhanga C, Neubig R, Pawson AJ, Pin JP, Sharman JL, Spedding M, Spindel E, Stoddart L, Storjohann L, Thomas WG, Tirupula K, Vanderheyden P. Class A Orphans in GtoPdb v.2023.1. IUPHAR/BPS Guide to Pharmacology CITE. 2023; 2023(1). Available from: https://doi.org/10.2218/gtopdb/F16/2023.1.