GPR75 is currently classified as an orphan GPCR and several studies are underway to identify its ligand. In one study, the chemokine CCL5 (RANTES) has been shown to stimulate calcium mobilization and inositol triphosphate formation in GPR75-transfected cells.[7]
A 2021 study by Akbari & Gilani et. al. reported that people with protein-truncating variants of GPR75 were associated with 5.3kg lower body weight and 54% lower odds for obesity. GPR75 knock-out mice showed resistance to weight gain under high-fat diet.[8]
References
^ a b cGRCh38: Ensembl release 89: ENSG00000119737 – Ensembl, May 2017
^ a b cGRCm38: Ensembl release 89: ENSMUSG00000043999 – Ensembl, May 2017
^"Human PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
^"Mouse PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
^Tarttelin EE, Kirschner LS, Bellingham J, Baffi J, Taymans SE, Gregory-Evans K, Csaky K, Stratakis CA, Gregory-Evans CY (June 1999). "Cloning and characterization of a novel orphan G-protein-coupled receptor localized to human chromosome 2p16". Biochemical and Biophysical Research Communications. 260 (1): 174–80. doi:10.1006/bbrc.1999.0753. PMID 10381362.
^ a b"Entrez Gene: GPR75 G protein-coupled receptor 75".
^Ignatov A, Robert J, Gregory-Evans C, Schaller HC (November 2006). "RANTES stimulates Ca2+ mobilization and inositol trisphosphate (IP3) formation in cells transfected with G protein-coupled receptor 75". British Journal of Pharmacology. 149 (5): 490–7. doi:10.1038/sj.bjp.0706909. PMC2014681. PMID 17001303.
^Akbari P, Gilani A, Sosina O, et al. (2 July 2021). "Sequencing of 640,000 exomes identifies GPR75 variants associated with protection from obesity". Science. 373 (6550). doi:10.1126/science.abf8683. PMC10275396. PMID 34210852. S2CID 235699731.