Growth hormone secretagogue receptor
Lua error in Module:Infobox_gene at line 33: attempt to index field 'wikibase' (a nil value). Growth hormone secretagogue receptor (GHSR), or ghrelin receptor, is a G protein-coupled receptor that binds ghrelin[1] and plays a role in energy homeostasis and regulation of body weight.[2] In the brain, they are located in the hypothalamic ventromedial nucleus and arcuate nucleus, as well as in ventral tegmental area dopamine neurons projecting to the nucleus accumbens.[3]
Contents
Function
Ghrelin is an appetite-regulating factor secreted from peripheral organs that is involved in regulation of energy homoeostasis via binding to the receptor resulting in the secretion of growth hormone by the pituitary gland.[4] The pathway activated by binding of ghrelin to the growth hormone secretagogue receptor, GHSR1a, regulates the activation of the downstream mitogen-activated protein kinase, Akt, nitric oxide synthase, and AMPK cascades in different cellular systems.[2] One of the important features of GHSR1a displays constitutive activity possessing basal activity in the absence of an agonist, resulting in a high degree of receptor internalization as well as of signaling activity.[2] Inverse agonists for the ghrelin receptor could be particularly interesting for the treatment of obesity.[5] This activity seems to provide a tonic signal required for the development of normal height, probably through an effect on the GH axis.[6]
Transcripts
Two identified transcript variants are expressed in several tissues and are evolutionary conserved in fish and swine. One transcript, 1a, excises an intron and encodes the functional protein; this protein is the receptor for the ghrelin ligand and defines a neuroendocrine pathway for growth hormone release. The second transcript (1b) retains the intron and does not function as a receptor for ghrelin; however, it may function to attenuate activity of isoform 1a.[7]
Selective ligands
A range of selective ligands for the GHSR receptor are now available and are being developed for several clinical applications. GHSR agonists have appetite-stimulating and growth hormone-releasing effects, and are likely to be useful for the treatment of muscle wasting and frailty associated with old-age and degenerative diseases. On the other hand, GHSR antagonists have anorectic effects and are likely to be useful for the treatment of obesity.
Agonists
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Antagonists
References
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Further reading
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External links
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- growth hormone secretagogue receptor at the US National Library of Medicine Medical Subject Headings (MeSH)
- Ghrelin at Colorado State University
This article incorporates text from the United States National Library of Medicine, which is in the public domain.
