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Integrating GHS into the Ghrelin System

Oligopeptide derivatives of metenkephalin were found to stimulate growth-hormone (GH) release directly by pituitary somatotrope cells in vitro in 1977. Members of this class of peptides and nonpeptidyl mimetics are referred to as GH secretagogues (GHSs). A specific guanosine triphosphatate-binding p...

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Autores principales: Veldhuis, Johannes D., Bowers, Cyril Y.
Formato: Texto
Lenguaje:English
Publicado: Hindawi Publishing Corporation 2010
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2925380/
https://www.ncbi.nlm.nih.gov/pubmed/20798846
http://dx.doi.org/10.1155/2010/879503
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author Veldhuis, Johannes D.
Bowers, Cyril Y.
author_facet Veldhuis, Johannes D.
Bowers, Cyril Y.
author_sort Veldhuis, Johannes D.
collection PubMed
description Oligopeptide derivatives of metenkephalin were found to stimulate growth-hormone (GH) release directly by pituitary somatotrope cells in vitro in 1977. Members of this class of peptides and nonpeptidyl mimetics are referred to as GH secretagogues (GHSs). A specific guanosine triphosphatate-binding protein-associated heptahelical transmembrane receptor for GHS was cloned in 1996. An endogenous ligand for the GHS receptor, acylghrelin, was identified in 1999. Expression of ghrelin and homonymous receptor occurs in the brain, pituitary gland, stomach, endothelium/vascular smooth muscle, pancreas, placenta, intestine, heart, bone, and other tissues. Principal actions of this peptidergic system include stimulation of GH release via combined hypothalamopituitary mechanisms, orexigenesis (appetitive enhancement), insulinostasis (inhibition of insulin secretion), cardiovascular effects (decreased mean arterial pressure and vasodilation), stimulation of gastric motility and acid secretion, adipogenesis with repression of fat oxidation, and antiapoptosis (antagonism of endothelial, neuronal, and cardiomyocyte death). The array of known and proposed interactions of ghrelin with key metabolic signals makes ghrelin and its receptor prime targets for drug development.
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spelling pubmed-29253802010-08-26 Integrating GHS into the Ghrelin System Veldhuis, Johannes D. Bowers, Cyril Y. Int J Pept Review Article Oligopeptide derivatives of metenkephalin were found to stimulate growth-hormone (GH) release directly by pituitary somatotrope cells in vitro in 1977. Members of this class of peptides and nonpeptidyl mimetics are referred to as GH secretagogues (GHSs). A specific guanosine triphosphatate-binding protein-associated heptahelical transmembrane receptor for GHS was cloned in 1996. An endogenous ligand for the GHS receptor, acylghrelin, was identified in 1999. Expression of ghrelin and homonymous receptor occurs in the brain, pituitary gland, stomach, endothelium/vascular smooth muscle, pancreas, placenta, intestine, heart, bone, and other tissues. Principal actions of this peptidergic system include stimulation of GH release via combined hypothalamopituitary mechanisms, orexigenesis (appetitive enhancement), insulinostasis (inhibition of insulin secretion), cardiovascular effects (decreased mean arterial pressure and vasodilation), stimulation of gastric motility and acid secretion, adipogenesis with repression of fat oxidation, and antiapoptosis (antagonism of endothelial, neuronal, and cardiomyocyte death). The array of known and proposed interactions of ghrelin with key metabolic signals makes ghrelin and its receptor prime targets for drug development. Hindawi Publishing Corporation 2010 2010-03-18 /pmc/articles/PMC2925380/ /pubmed/20798846 http://dx.doi.org/10.1155/2010/879503 Text en Copyright © 2010 J. D. Veldhuis and C. Y. Bowers. https://creativecommons.org/licenses/by/3.0/ This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Review Article
Veldhuis, Johannes D.
Bowers, Cyril Y.
Integrating GHS into the Ghrelin System
title Integrating GHS into the Ghrelin System
title_full Integrating GHS into the Ghrelin System
title_fullStr Integrating GHS into the Ghrelin System
title_full_unstemmed Integrating GHS into the Ghrelin System
title_short Integrating GHS into the Ghrelin System
title_sort integrating ghs into the ghrelin system
topic Review Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2925380/
https://www.ncbi.nlm.nih.gov/pubmed/20798846
http://dx.doi.org/10.1155/2010/879503
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