グレリン受容体、グレリンレセプター

WordNet

a cellular structure that is postulated to exist in order to mediate between a chemical agent that acts on nervous tissue and the physiological response
a gastrointestinal hormone produced by epithelial cells lining the fundus of the stomach; appears to be a stimulant for appetite and feeding, but is also a strong stimulant of growth hormone secretion from the anterior pituitary

PrepTutorEJDIC

=sense organ / 受信装置

Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2013/10/18 14:20:27」(JST)

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Growth hormone secretagogue receptor is a G protein-coupled receptor that binds ghrelin^[1] and plays a role in energy homeostasis and regulation of body weight.^[2]

Function[edit]

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. ^[3] 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.^[4] This activity seems to provide a tonic signal required for the development of normal height, probably through an effect on the GH axis.^[5]

Transcripts[edit]

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.^[6]

Selective ligands[edit]

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[edit]

Capromorelin
GHRP-2
GHRP-6
Hexarelin
Ipamorelin
MK-677
SM-130,686
Tabimorelin

Antagonists[edit]

A-778,193

References[edit]

^ Davenport AP, Bonner TI, Foord SM, Harmar AJ, Neubig RR, Pin JP, Spedding M, Kojima M, Kangawa K (2005). "International Union of Pharmacology. LVI. Ghrelin receptor nomenclature, distribution, and function". Pharmacol. Rev. 57 (4): 541–6. doi:10.1124/pr.57.4.1. PMID 16382107.
^ ^a ^b ^c Pazos Y, Casanueva FF, Camiña JP (2007). "Basic aspects of ghrelin action". Vitam. Horm. 77: 89–119. doi:10.1016/S0083-6729(06)77005-4. PMID 17983854.
^ Wren AM, Small CJ, Ward HL, et al. (November 2000). "The novel hypothalamic peptide ghrelin stimulates food intake and growth hormone secretion". Endocrinology 141 (11): 4325–8. doi:10.1210/en.141.11.4325. PMID 11089570.
^ Holst B, Cygankiewicz A, Jensen TH, Ankersen M, Schwartz TW (2003). "High constitutive signaling of the ghrelin receptor--identification of a potent inverse agonist". Mol. Endocrinol. 17 (11): 2201–10. doi:10.1210/me.2003-0069. PMID 12907757.
^ Pantel J, Legendre M, Cabrol S, Hilal L, Hajaji Y, Morisset S, Nivot S, Vie-Luton MP, Grouselle D, de Kerdanet M, Kadiri A, Epelbaum J, Le Bouc Y, Amselem S (2006). "Loss of constitutive activity of the growth hormone secretagogue receptor in familial short stature". J Clin Invest. 116 (3): 760–8. doi:10.1172/JCI25303. PMC 1386106. PMID 16511605.
^ "Entrez Gene: GHSR growth hormone secretagogue receptor".

External links[edit]

"Ghrelin Receptor". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.
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.

This transmembrane receptor-related article is a stub. You can help Wikipedia by expanding it.

UpToDate Contents

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1. グレリン ghrelin
2. 成長ホルモンの生理学 physiology of growth hormone
3. 癌における食欲不振および悪液質の薬理学的マネージメント pharmacologic management of cancer anorexia cachexia
4. 肥満への遺伝的影響と病態生理 genetic contribution and pathophysiology of obesity
5. ソマトスタチンの生理学とその類縁体 physiology of somatostatin and its analogues

English Journal

Food restriction, ghrelin, its antagonist and obestatin control expression of ghrelin and its receptor in chicken hypothalamus and ovary.

Sirotkin AV, Pavlova S, Tena-Sempere M, Grossmann R, Jiménez MR, Rodriguez JM, Valenzuela F.SourceDept. Genetics and Reproduction, Research Centre of Animal Production, Hlohovecká 2, 949 92 Luzianky, Slovakia; Dept. Zoology and Anthropology, Constantine the Philosopher University, 949 74 Nitra, Slovakia. Electronic address: sirotkin@cvzv.sk.
Comparative biochemistry and physiology. Part A, Molecular & integrative physiology.Comp Biochem Physiol A Mol Integr Physiol.2013 Jan;164(1):141-53. doi: 10.1016/j.cbpa.2012.07.010. Epub 2012 Aug 1.
The purpose of the present study was to identify the role of age, nutritional state and some metabolic hormones in control of avian hypothalamic and ovarian ghrelin/ghrelin receptor system. We examined the effect of food restriction, administration of ghrelin 1-18, ghrelin antagonistic analogue (D-L
PMID 22877785

Neurocircuitry involved in the development of alcohol addiction: the dopamine system and its access points.

Söderpalm B, Ericson M.SourceAddiction Biology Unit, Section of Psychiatry and Neurochemistry, Institute of Neuroscience and Physiology Sahlgrenska Academy, University of Gothenburg, Gothenburg, Sweden. bo.soderpalm@neuro.gu.se
Current topics in behavioral neurosciences.Curr Top Behav Neurosci.2013;13:127-61. doi: 10.1007/7854_2011_170.
The brain reward system, and especially the mesolimbic dopamine pathway, plays a major role in drug reinforcement and is most likely involved in the development of drug addiction. All major drugs of abuse, including ethanol, acutely activate the mesolimbic dopamine system. Both this acute drug-induc
PMID 22094880

Japanese Journal

グレリン受容体 : リガンド非依存性の恒常的活性化とその異常 (第5土曜特集 GPCR研究の最前線2016) -- (GPCR機能の新展開)

医学のあゆみ 256(5), 519-523, 2016-01-30
NAID 40020717002

Effects of retinoic acid on growth hormone-releasing hormone receptor, growth hormone secretagogue receptor gene expression and growth hormone secretion in rat anterior pituitary cells

Endocrine Journal 63(6), 555-561, 2016
NAID 130005159557

Effects of retinoic acid on growth hormone-releasing hormone receptor, growth hormone secretagogue receptor gene expression and growth hormone secretion in rat anterior pituitary cells

Endocrine Journal advpub(0), 2016
NAID 130005143578

「グレリン受容体」

Growth hormone secretagogue receptor
Identifiers
Symbol	GHSR
External IDs	OMIM: 601898 MGI: 2441906 HomoloGene: 57161 IUPHAR: ghrelin receptor ChEMBL: 4616 GeneCards: GHSR Gene
Gene Ontology
Molecular function	• growth hormone secretagogue receptor activity; • G-protein coupled receptor activity; • growth hormone-releasing hormone receptor activity; • peptide hormone binding;
Cellular component	• plasma membrane; • cell surface; • integral to membrane; • neuron projection; • membrane raft;
Biological process	• G-protein coupled receptor signaling pathway; • actin polymerization or depolymerization; • adult feeding behavior; • response to hormone stimulus; • hormone-mediated signaling pathway; • growth hormone secretion; • response to food; • positive regulation of appetite; • negative regulation of interleukin-1 beta production; • cellular response to insulin stimulus; • positive regulation of multicellular organism growth; • negative regulation of tumor necrosis factor biosynthetic process; • regulation of hindgut contraction; • positive regulation of insulin-like growth factor receptor signaling pathway; • negative regulation of interleukin-6 biosynthetic process; • positive regulation of fatty acid metabolic process; • negative regulation of insulin secretion; • decidualization; • negative regulation of inflammatory response; • regulation of synapse assembly;
	Sources: Amigo / QuickGO
RNA expression pattern
	More reference expression data
Orthologs
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　　[★]

英: ghrelin receptor
関: グレリンレセプター

「グレリンレセプター」

　　[★]

英: ghrelin receptor
関: グレリン受容体

[pmid16382107-1] Davenport AP, Bonner TI, Foord SM, Harmar AJ, Neubig RR, Pin JP, Spedding M, Kojima M, Kangawa K (2005). "International Union of Pharmacology. LVI. Ghrelin receptor nomenclature, distribution, and function". Pharmacol. Rev. 57 (4): 541–6. doi:10.1124/pr.57.4.1. PMID 16382107.

[pazos2007-2] Pazos Y, Casanueva FF, Camiña JP (2007). "Basic aspects of ghrelin action". Vitam. Horm. 77: 89–119. doi:10.1016/S0083-6729(06)77005-4. PMID 17983854.

[3] Wren AM, Small CJ, Ward HL, et al. (November 2000). "The novel hypothalamic peptide ghrelin stimulates food intake and growth hormone secretion". Endocrinology 141 (11): 4325–8. doi:10.1210/en.141.11.4325. PMID 11089570.

[4] Holst B, Cygankiewicz A, Jensen TH, Ankersen M, Schwartz TW (2003). "High constitutive signaling of the ghrelin receptor--identification of a potent inverse agonist". Mol. Endocrinol. 17 (11): 2201–10. doi:10.1210/me.2003-0069. PMID 12907757.

[5] Pantel J, Legendre M, Cabrol S, Hilal L, Hajaji Y, Morisset S, Nivot S, Vie-Luton MP, Grouselle D, de Kerdanet M, Kadiri A, Epelbaum J, Le Bouc Y, Amselem S (2006). "Loss of constitutive activity of the growth hormone secretagogue receptor in familial short stature". J Clin Invest. 116 (3): 760–8. doi:10.1172/JCI25303. PMC 1386106. PMID 16511605.

[entrez-6] "Entrez Gene: GHSR growth hormone secretagogue receptor".

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ghrelin receptor