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IUPHAR Nomenclature Report

International Union of Pharmacology. LVI. Ghrelin Receptor Nomenclature, Distribution, and Function

Clinical Pharmacology Unit, University of Cambridge, Cambridge, United Kingdom (A.P.D.); Laboratory of Genetics, National Institute of Mental Health, Bethesda, Maryland (T.I.B.); GlaxoSmithKline Research and Development, Stevenage, Hertfordshire, United Kingdom (S.M.F.); Division of Neuroscience and Centre for Neuroscience Research, University of Edinburgh, Edinburgh, United Kingdom (A.J.H.); Department of Pharmacology, University of Michigan, Ann Arbor, Michigan (R.R.N.); Centre National de la Recherche Scientifique, Montpellier, France (J.-P.P.); Institut de Recherches Internationales Servier (I.R.I.S.), Neuilly-sur-Seine, France (M.S.); and National Cardiovascular Center Research Institute, Suita, Osaka, Japan (M.K., K.K.)

Abstract

I. Introduction

II. Growth Hormone Secretagogue Receptor 1a Designated as the Ghrelin Receptor

III. Distribution of Receptor and mRNA Encoding the Receptor

IV. Radiolabeled Ligands

V. Agonists

VI. Antagonists

VII. Physiological Role

VIII. Pathophysiological Role

IX. Genetically Modified Animals

A. Ghrelin Receptor

B. Peptide

Ghrelin is a 28-amino acid peptide originally isolated from rat stomach and is cleaved from a 117-amino acid precursor. The sequence of the mature peptide from rats and mice differs by two amino acids from that of human ghrelin. Alternative splicing of the ghrelin gene transcript can result in the translation of a second biologically active peptide, des-Gln¹⁴-ghrelin. Both peptides have a unique post-translational modification, octanoylation of Ser³, which is essential for the binding to receptors in hypothalamus and pituitary and stimulating the release of growth hormone from the pituitary. The growth hormone secretagogue receptor (GHS-R1a, Swiss-Prot code Q92847, LocusLink ID 2693), a rhodopsin-like seven transmembrane spanning G protein-coupled receptors belonging to Family A, was cloned in 1996 from the pituitary and hypothalamus and shown to be the target of growth hormone secretagogues (GHS), a class of synthetic peptide and nonpeptide compounds causing growth hormone release from the anterior pituitary. In 1999, ghrelin was identified as the endogenous cognate ligand for this receptor. The purpose of this review is to propose an official International Union of Pharmacology Committee on Receptor Nomenclature and Drug Classification (NC-IUPHAR) nomenclature designating GHS-R1a as the ghrelin receptor to follow the convention of naming receptors after the endogenous agonist, abbreviated where necessary to GRLN.

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