Ghrelin receptor

Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).

Overview

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Ghrelin receptors [3] are activated by a 28 amino-acid peptide originally isolated from rat stomach, where it is cleaved from a 117 amino-acid precursor (GHRL, Q9UBU3). The human gene encoding the precursor peptide has 83% sequence homology to rat prepro-ghrelin, although the mature peptides from rat and human differ by only two amino acids [11]. Alternative splicing results in the formation of a second peptide, [des-Gln14]ghrelin (GHRL, Q9UBU3) with equipotent biological activity [8]. A unique post-translational modification (octanoylation of Ser3, catalysed by ghrelin Ο-acyltransferase (MBOAT4, Q96T53) [17] occurs in both peptides, essential for full activity in binding to the ghrelin receptors in the hypothalamus and pituitary; and the release of growth hormone release from the pituitary [10]. Structure activity studies showed the first five N-terminal amino acids to be the minimum required for binding [2], and receptor mutagenesis has indicated overlap of the ghrelin binding site with those for small molecule agonists and allosteric modulators of ghrelin (GHRL, Q9UBU3) function [6]. In cell systems, the ghrelin receptor is constitutively active [7], but this is abolished by a naturally occurring mutation (A204E) that results in decreased cell surface receptor expression and is associated with familial short stature [14].

Receptors

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How to cite this family page

Database page citation:

Ghrelin receptor. Accessed on 01/10/2014. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=28.

Concise Guide to PHARMACOLOGY citation:

Alexander SPH, Benson HE, Faccenda E, Pawson AJ, Sharman JL, Spedding M, Peters JA and Harmar AJ, CGTP Collaborators. (2013) The Concise Guide to PHARMACOLOGY 2013/14: G Protein-Coupled Receptors. Br J Pharmacol. 170: 1459–1581.