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Seven Transmembrane G Protein-Coupled Receptor Repertoire of Gastric Ghrelin Cells

Seven Transmembrane G Protein-Coupled Receptor Repertoire of Gastric Ghrelin Cells

Maja S Engelstoft, Won-Mee Park, Ichiro Sakata, Line V Kristensen, Anna Sofie Husted, Sherri Osborne-Lawrence, Paul K Piper, Angela K Walker, Maria H Pedersen, Mark K Nøhr, Jie Pan, Christopher J Sinz, etc.

Mol Metab. 2013 Sep 4;2(4):376-92.

PMID: 24327954

Abstract:

The molecular mechanisms regulating secretion of the orexigenic-glucoregulatory hormone ghrelin remain unclear. Based on qPCR analysis of FACS-purified gastric ghrelin cells, highly expressed and enriched 7TM receptors were comprehensively identified and functionally characterized using in vitro, ex vivo and in vivo methods. Five Gαs-coupled receptors efficiently stimulated ghrelin secretion: as expected the β1-adrenergic, the GIP and the secretin receptors but surprisingly also the composite receptor for the sensory neuropeptide CGRP and the melanocortin 4 receptor. A number of Gαi/o-coupled receptors inhibited ghrelin secretion including somatostatin receptors SSTR1, SSTR2 and SSTR3 and unexpectedly the highly enriched lactate receptor, GPR81. Three other metabolite receptors known to be both Gαi/o- and Gαq/11-coupled all inhibited ghrelin secretion through a pertussis toxin-sensitive Gαi/o pathway: FFAR2 (short chain fatty acid receptor; GPR43), FFAR4 (long chain fatty acid receptor; GPR120) and CasR (calcium sensing receptor). In addition to the common Gα subunits three non-common Gαi/o subunits were highly enriched in ghrelin cells: GαoA, GαoB and Gαz. Inhibition of Gαi/o signaling via ghrelin cell-selective pertussis toxin expression markedly enhanced circulating ghrelin. These 7TM receptors and associated Gα subunits constitute a major part of the molecular machinery directly mediating neuronal and endocrine stimulation versus metabolite and somatostatin inhibition of ghrelin secretion including a series of novel receptor targets not previously identified on the ghrelin cell.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP53984364	3-Chloro-5-hydroxybenzoic acid		53984-36-4	Price

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