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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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Formato: | Texto |
Lenguaje: | English |
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Hindawi Publishing Corporation
2010
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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. |
format | Text |
id | pubmed-2925380 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2010 |
publisher | Hindawi Publishing Corporation |
record_format | MEDLINE/PubMed |
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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