Ghrelin Receptor Antibodies
The ghrelin receptor (GHS-R1a), encoded by GHSR, is a class A G protein-coupled receptor activated by acylated ghrelin, a peptide produced predominantly by the stomach. Ghrelin requires an acyl modification at serine 3, usually an octanoyl group, for potent activation of the receptor. GHS-R1a couples primarily to Gq/11, activating phospholipase C and increasing intracellular calcium. It is expressed in pituitary somatotrophs and selected brain regions, including the hypothalamus, where it contributes to growth hormone release, appetite, and energy homeostasis. The receptor exhibits substantial constitutive activity in experimental systems, allowing signaling in the absence of ghrelin. Agonist stimulation can induce receptor phosphorylation, β-arrestin recruitment, and internalization, while constitutive internalization can also occur independently of β-arrestins. Macimorelin, an oral ghrelin receptor agonist, is approved for the diagnosis of adult growth hormone deficiency. Anamorelin, another oral agonist, is approved in Japan for cancer-associated cachexia. Ghrelin receptors are regulated by phosphorylation of carboxyl-terminal serine362/serine363 (pS362/pS363-GHSR). This nomenclature refers to the human Ghrelin receptor. This phosphorylation motif is conserved across species but corresponds to pS360/pS361-GHSR in mice and rats. For more information on ghrelin receptor pharmacology please refer to the IUPHAR database. For further reading refer to:
Davenport AP, Bonner TI, Foord SM, Harmar AJ, Neubig RR, Pin JP, Spedding M, Kojima M, Kangawa K. International Union of Pharmacology. LVI. Ghrelin receptor nomenclature, distribution, and function. Pharmacol Rev. 2005 Dec;57(4):541-6. doi: 10.1124/pr.57.4.1. PMID: 16382107.
Ge X, Yang H, Bednarek MA, Galon-Tilleman H, Chen P, Chen M, Lichtman JS, Wang Y, Dalmas O, Yin Y, Tian H, Jermutus L, Grimsby J, Rondinone CM, Konkar A, Kaplan DD. LEAP2 Is an Endogenous Antagonist of the Ghrelin Receptor. Cell Metab. 2018 Feb 6;27(2):461-469.e6. doi: 10.1016 j.cmet.2017.10.016. PMID: 29233536.