Historical Background
Growth hormone secretagogue receptor (GHSR) was first cloned from human hypothalamus and pituitary, with the function of binding growth hormone secretagogue (Howard et al. 1996). Both peptidyl and nonpeptidyl growth hormone secretagogues could activate the GHSR on membrane of somatotroph cells from anterior-pituitary (McKee et al. 1997). Three years later, its endogenous ligand was found in rat stomach extract by Kojima et al. This endogenous ligand for GHSR was named as ghrelin because ghr is the Proto-Indo-European root for grow (Kojima et al. 1999).
GHSR plays important roles in many canonical physiological functions when activated by its endogenous ligand ghrelin. Ghrelin is a 28 amino acid peptide released into blood in response to hormonal or neural signals. Activation of GHSR requires a unique octanoylation of the third amino acid serine of ghrelin. The...
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References
Chen C, Zhang J, Vincent JD, Israel JM. Two types of voltage-dependent calcium current in rat somatotrophs are reduced by somatostatin. J Physiol. 1990;425:29–42.
Doi A, Shono T, Nishi M, Furuta H, Sasaki H, Nanjo K. IA-2beta, but not IA-2, is induced by ghrelin and inhibits glucose-stimulated insulin secretion. Proc Natl Acad Sci USA. 2006;103(4):885–90.
Howard AD, Feighner SD, Cully DF, Arena JP, Liberator PA, Rosenblum CI, et al. A receptor in pituitary and hypothalamus that functions in growth hormone release. Science. 1996;273(5277):974–7.
Kim MS, Yoon CY, Jang PG, Park YJ, Shin CS, Park HS, et al. The mitogenic and antiapoptotic actions of ghrelin in 3 T3-L1 adipocytes. Mol Endocrinol. 2004;18(9):2291–301.
Kohno D, Gao HZ, Muroya S, Kikuyama S, Yada T. Ghrelin directly interacts with neuropeptide-Y-containing neurons in the rat arcuate nucleus: Ca2+ signaling via protein kinase A and N-type channel-dependent mechanisms and cross-talk with leptin and orexin. Diabetes. 2003;52(4):948–56.
Kojima M, Hosoda H, Date Y, Nakazato M, Matsuo H, Kangawa K. Ghrelin is a growth-hormone-releasing acylated peptide from stomach. Nature. 1999;402(6762):656–60.
Li Z, Xu G, Qin Y, Zhang C, Tang H, Yin Y, et al. Ghrelin promotes hepatic lipogenesis by activation of mTOR-PPARgamma signaling pathway. Proc Natl Acad Sci USA. 2014;111(36):13163–8.
McKee KK, Palyha OC, Feighner SD, Hreniuk DL, Tan CP, Phillips MS, et al. Molecular analysis of rat pituitary and hypothalamic growth hormone secretagogue receptors. Mol Endocrinol. 1997;11(4):415–23.
Murata M, Okimura Y, Iida K, Matsumoto M, Sowa H, Kaji H, et al. Ghrelin modulates the downstream molecules of insulin signaling in hepatoma cells. J Biol Chem. 2002;277(7):5667–74.
Nakazato M, Murakami N, Date Y, Kojima M, Matsuo H, Kangawa K, et al. A role for ghrelin in the central regulation of feeding. Nature. 2001;409(6817):194–8.
Pedretti A, Villa M, Pallavicini M, Valoti E, Vistoli G. Construction of human ghrelin receptor (hGHS-R1a) model using a fragmental prediction approach and validation through docking analysis. J Med Chem. 2006;49(11):3077–85.
Petersenn S. Structure and regulation of the growth hormone secretagogue receptor. Minerva Endocrinol. 2002;27(4):243–56.
Petersenn S, Rasch AC, Penshorn M, Beil FU, Schulte HM. Genomic structure and transcriptional regulation of the human growth hormone secretagogue receptor. Endocrinology. 2001;142(6):2649–59.
Schwartz TW, Frimurer TM, Holst B, Rosenkilde MM, Elling CE. Molecular mechanism of 7TM receptor activation – a global toggle switch model. Annu Rev Pharmacol Toxicol. 2006;46:481–519.
Stevanovic D, Janjetovic K, Misirkic M, Vucicevic L, Sumarac-Dumanovic M, Micic D, et al. Intracerebroventricular administration of metformin inhibits ghrelin-induced hypothalamic AMP-kinase signalling and food intake. Neuroendocrinology. 2012;96(1):24–31.
Stoyanova II. Ghrelin: a link between ageing, metabolism and neurodegenerative disorders. Neurobiol Dis. 2014;72(Pt A):72–83.
Theander-Carrillo C, Wiedmer P, Cettour-Rose P, Nogueiras R, Perez-Tilve D, Pfluger P, et al. Ghrelin action in the brain controls adipocyte metabolism. J Clin Invest. 2006;116(7):1983–93.
Tschop M, Smiley DL, Heiman ML. Ghrelin induces adiposity in rodents. Nature. 2000;407(6806):908–13.
Xu G, Wang Z, Li Y, Li Z, Tang H, Zhao J, et al. Ghrelin contributes to derangements of glucose metabolism induced by rapamycin in mice. Diabetologia. 2012;55(6):1813–23.
Yin Y, Li Y, Zhang W. The growth hormone secretagogue receptor: its intracellular signaling and regulation. Int J Mol Sci. 2014;15:4837–55.
Acknowledgments
This work was supported by grants from the National Natural Science Foundation of China (81330010, 81390354) and American Diabetes Association grant #1-13-BS-225.
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Yin, Y., Liu, S., Zhang, W. (2018). GHSR: Growth Hormone Secretagogue Receptor. In: Choi, S. (eds) Encyclopedia of Signaling Molecules. Springer, Cham. https://doi.org/10.1007/978-3-319-67199-4_101611
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DOI: https://doi.org/10.1007/978-3-319-67199-4_101611
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