Growth hormone secretagogue receptor

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Growth hormone secretagogue receptor
Identifiers
Symbols GHSR;
External IDs OMIM: 601898 MGI: 2441906 HomoloGene: 57161
RNA expression pattern

More reference expression data
Orthologs
Human Mouse
Entrez 2693 208188
Ensembl ENSG00000121853 ENSMUSG00000051136
Uniprot Q92847 Q0VBE5
Refseq NM_004122 (mRNA)
NP_004113 (protein)		 NM_177330 (mRNA)
NP_796304 (protein)
Location Chr 3: 173.65 - 173.65 Mb Chr 3: 27.56 - 27.57 Mb
Pubmed search [1] [2]


Growth hormone secretagogue receptor is a G protein-coupled receptor which binds ghrelin.[1]

This gene encodes a member of the G-protein coupled receptor family. The encoded protein may play a role in energy homeostasis and regulation of body weight.[2] 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.[3] This activity seems to provide a tonic signal required for the development of normal height, probably through an effect on the GH axis.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.[4]


References

  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. 
  2. ^ 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. 
  3. ^ 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. 
  4. ^ "Entrez Gene: GHSR growth hormone secretagogue receptor".

Further reading

  • Smith RG, Leonard R, Bailey AR, et al. (2001). "Growth hormone secretagogue receptor family members and ligands.". Endocrine 14 (1): 9–14. PMID 11322507. 
  • Petersenn S (2003). "Structure and regulation of the growth hormone secretagogue receptor.". Minerva Endocrinol. 27 (4): 243–56. PMID 12511847. 
  • Holst B, Schwartz TW (2006). "Ghrelin receptor mutations--too little height and too much hunger.". J. Clin. Invest. 116 (3): 637–41. doi:10.1172/JCI27999. PMID 16511600. 
  • Nogueiras R, Perez-Tilve D, Wortley KE, Tschöp M (2006). "Growth hormone secretagogue (ghrelin-) receptors--a complex drug target for the regulation of body weight.". CNS & neurological disorders drug targets 5 (3): 335–43. PMID 16787234. 
  • Engbaek K (1978). "[Giardia lamblia and other intestinal parasites in children in day-institutions. Incidence and significance]". Ugeskr. Laeg. 140 (1): 14–7. PMID 601898. 
  • Howard AD, Feighner SD, Cully DF, et al. (1996). "A receptor in pituitary and hypothalamus that functions in growth hormone release.". Science 273 (5277): 974–7. PMID 8688086. 
  • McKee KK, Palyha OC, Feighner SD, et al. (1997). "Molecular analysis of rat pituitary and hypothalamic growth hormone secretagogue receptors.". Mol. Endocrinol. 11 (4): 415–23. PMID 9092793. 
  • Kaji H, Tai S, Okimura Y, et al. (1999). "Cloning and characterization of the 5'-flanking region of the human growth hormone secretagogue receptor gene.". J. Biol. Chem. 273 (51): 33885–8. PMID 9852035. 
  • Kojima M, Hosoda H, Date Y, et al. (2000). "Ghrelin is a growth-hormone-releasing acylated peptide from stomach.". Nature 402 (6762): 656–60. doi:10.1038/45230. PMID 10604470. 
  • Deghenghi R, Papotti M, Ghigo E, Muccioli G (2001). "Cortistatin, but not somatostatin, binds to growth hormone secretagogue (GHS) receptors of human pituitary gland.". J. Endocrinol. Invest. 24 (1): RC1–3. PMID 11227737. 
  • Tannenbaum GS, Bowers CY (2001). "Interactions of growth hormone secretagogues and growth hormone-releasing hormone/somatostatin.". Endocrine 14 (1): 21–7. PMID 11322498. 
  • Petersenn S, Rasch AC, Penshorn M, et al. (2001). "Genomic structure and transcriptional regulation of the human growth hormone secretagogue receptor.". Endocrinology 142 (6): 2649–59. PMID 11356716. 
  • Shuto Y, Shibasaki T, Otagiri A, et al. (2002). "Hypothalamic growth hormone secretagogue receptor regulates growth hormone secretion, feeding, and adiposity.". J. Clin. Invest. 109 (11): 1429–36. PMID 12045256. 
  • Strausberg RL, Feingold EA, Grouse LH, et al. (2003). "Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences.". Proc. Natl. Acad. Sci. U.S.A. 99 (26): 16899–903. doi:10.1073/pnas.242603899. PMID 12477932. 
  • Gaytan F, Barreiro ML, Chopin LK, et al. (2003). "Immunolocalization of ghrelin and its functional receptor, the type 1a growth hormone secretagogue receptor, in the cyclic human ovary.". J. Clin. Endocrinol. Metab. 88 (2): 879–87. PMID 12574228. 
  • Dass NB, Munonyara M, Bassil AK, et al. (2003). "Growth hormone secretagogue receptors in rat and human gastrointestinal tract and the effects of ghrelin.". Neuroscience 120 (2): 443–53. PMID 12890514. 
  • Lall S, Balthasar N, Carmignac D, et al. (2004). "Physiological studies of transgenic mice overexpressing growth hormone (GH) secretagogue receptor 1A in GH-releasing hormone neurons.". Endocrinology 145 (4): 1602–11. doi:10.1210/en.2003-1509. PMID 14701677. 
  • Wang HJ, Geller F, Dempfle A, et al. (2004). "Ghrelin receptor gene: identification of several sequence variants in extremely obese children and adolescents, healthy normal-weight and underweight students, and children with short normal stature.". J. Clin. Endocrinol. Metab. 89 (1): 157–62. PMID 14715843. 

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v • d • e
Transmembrane receptor: G protein-coupled receptors
Class A: Rhodopsin like
α1 (A, B, D) • α2 (A, B, C) • β1 • β2 • β3
CysLT (1, 2) • LTB4 (1, 2) • FPRL1 • OXE • Prostaglandin (DP, EP (1, 2, 3, 4), PGF) • Prostacyclin • Thromboxane
B/W (1, 2) • FF (1, 2) • S • Y (1, 2, 4, 5)
GPR (1, 3, 4, 6, 12, 15, 17, 18, 19, 20, 21, 22, 23, 25, 26, 27, 31, 32, 33, 34, 35, 37, 39, 42, 44, 45, 50, 52, 55, 61, 62, 63, 65, 68, 75, 77, 78, 79, 82, 83, 84, 85, 87, 88, 92, 101, 103, 119, 120, 132, 135, 139, 141, 142, 146, 148, 149, 150, 151, 152, 153, 160, 161, 162, 171, 172, 173, 174, 176, 177, 182)
Adenosine (A1, A2a, A2b, A3) • P2Y (1, 2, 4, 5, 6, 8, 9, 10, 11, 12, 13, 14)
(all but 5-HT3) 5-HT1 (A, B, D, E, F) • 5-HT2 (A, B, C) • 5-HT (4, 5A, 6, 7)
Other
Acetylcholine (M1, M2, M3, M4, M5) • Adrenomedullin • Anaphylatoxin (C3a, C5a) • Angiotensin (1, 2) • Apelin • Bile acid • Bombesin (BRS3, GRPR, NMBR) • Bradykinin (B1, B2) • Cannabinoid (CB1, CB2) • Chemokine • Cholecystokinin (A, B) • Dopamine (D1, D2, D3, D4, D5) • EBI2 • Endothelin (A, B) • Estrogen • Formyl peptide (1, L1, L2) • Free fatty acid (1, 2, 3, 4) • FSH • Galanin (1, 2, 3) • Gonadotropin-releasing hormone (1, 2) • Ghrelin • Histamine (H1, H2, H3, H4) • Kisspeptin • Luteinizing hormone/choriogonadotropin • Lysophospholipid (1, 2, 3, 4, 5, 6, 7, 8) • MAS (1, 1L, D, E, F, G, X1, X2, X3, X4) • Melanocortin (1, 2, 3, 4, 5) • MCHR (1, 2) • Melatonin (1A, 1B) • Motilin • Neuromedin (B, U (1, 2)) • Neurotensin (1, 2) • Opioid (Delta, Kappa, Mu, Nociceptin, but not Sigma) • Olfactory • Opsin (3, 4, 5, 1LW, 1MW, 1SW, RGR, RRH) • Orexin (1, 2) • Oxytocin • Oxoglutarate • PAF • Prokineticin (1, 2) • Prolactin-releasing peptide • Protease-activated (1, 2, 3, 4) • Relaxin (1, 2, 3, 4) • Somatostatin (1, 2, 3, 4, 5) • SREB • Succinate • TAAR (1, 2, 3, 5, 6, 8, 9) • Tachykinin (1, 2, 3) • Thyrotropin • Thyrotropin-releasing hormone • Urotensin-II • Vasopressin (1A, 1B, 2)
Class B: Secretin like
GPR (56, 64, 97, 98, 110, 111, 112, 113, 114, 115, 116, 123, 124, 125, 126, 128, 133, 143, 144, 157)
Other
Class C: Metabotropic
glutamate / pheromone
TAS1R (1, 2, 3) • TAS2R (1, 3, 4, 5, 8, 9, 10, 12, 13, 14, 16, 38, 39, 40, 41, 43, 44, 45, 46, 47, 48, 49, 50)
Other
Calcium-sensing receptor • GABA B (1, 2) • Glutamate receptor (Metabotropic glutamate (1, 2, 3, 4, 5, 6, 7, 8)) • GPRC6A • GPR (156, 158, 179) • RAIG (1, 2, 3, 4)
Frizzled / Smoothened
Frizzled (1, 2, 3, 4, 5, 6, 7, 8, 9, 10) • Smoothened

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