Growth hormone-releasing hormone as an agonist of the ghrelin receptor GHS-R1a

Proceedings of the National Academy of Sciences of the United States of America

Volumn 105, Issue 51, 2008, Pages 20452-20457

  Casanueva, Felipe F ^a,b,c   Camiña, Jesus P ^a,c   Carreira, Marcos C ^c   Pazos, Yolanda ^a,c   Varga, Jozsef L ^d,e   Schally, Andrew V ^d,e  

^a HOSPITAL CLÍNICO UNIVERSITARIO   (Spain)

^b UNIVERSITY OF SANTIAGO DE COMPOSTELA   (Spain)

^c INSTITUTO DE SALUD CARLOS III   (Spain)

^d VETERANS AFFAIRS MEDICAL CENTER   (United States)

^e UNIVERSITY OF MIAMI MILLER SCHOOL OF MEDICINE   (United States)

Author keywords

Ghrelin; Ghrelin receptor; GHRH

Indexed keywords

GHRELIN RECEPTOR; GREEN FLUORESCENT PROTEIN; GROWTH HORMONE RELEASING FACTOR; INOSITOL PHOSPHATE;

ARTICLE; CALCIUM MOBILIZATION; CELL STRAIN HEK293; CHO CELL; CONFOCAL MICROSCOPY; CONTROLLED STUDY; ELECTRIC POTENTIAL; ENDOCYTOSIS; GENETIC TRANSFECTION; HUMAN; HUMAN CELL; LIGAND BINDING; PRIORITY JOURNAL; PROTEIN BINDING;

CALCIUM SIGNALING; CELL LINE; ENDOCYTOSIS; GROWTH HORMONE; GROWTH HORMONE-RELEASING HORMONE; HUMANS; INOSITOL PHOSPHATES; PROTEIN BINDING; RECEPTORS, GHRELIN; SIGNAL TRANSDUCTION; TRANSFECTION;

EID: 58149503669     PISSN: 00278424     EISSN: 10916490     Source Type: Journal    
DOI: 10.1073/pnas.0811680106     Document Type: Article

References (38)

1. Kojima M, Hosoda H, Date Y, Nakazato M, Matsuo H, Kangawa K (1999) Ghrelin is a growth-hormone-releasing acylated peptide from stomach. Nature 402:656-660.
2. van der Lely AJ, Tschöp M, Heiman ML, Ghigo E (2004) Biological, physiological, pathophysiological, and pharmacological aspects of ghrelin. Endocr Rev 25:426-457.
3. Murphy KG, Dhillo WS, Bloom SR (2006) Gut peptides in the regulation of food intake and energy homeostasis. Endocr Rev 27:719-727.
4. Wiedmer P, Nogueiras R, Broglio F, D'Alessio D, Tschöp MH (2007) Ghrelin, obesity and diabetes. Nat Clin Pract Endocrinol Metab 3:705-712.
5. Bowers CY, Reynolds GA, Durham D, Barrera CM, Pezzoli SS, Thorner MO (1990) Growth hormone (GH)-releasing peptide stimulates GH release in normal men and acts synergistically with GH-releasing hormone. J Clin Endocrinol Metab 70:975-982.
6. Hataya Y, Akamizu T, Takaya K, Kanamoto N, Ariyasu H, et al (2001) A low dose of ghrelin stimulates growth hormone (GH) release synergistically with GH-releasing hormone in humans. J Clin Endocrinol Metab 86:4552.
7. Peñalva A, Carballo A, Pombo M, Casanueva FF, Dieguez C (1993) Effect of growth hormone (GH)-releasing hormone (GHRH), atropine, pyridostigmine, or hypoglycemia on GHRP-6-induced GH secretion in man. J Clin Endocrinol Metab 76:168-171.
8. Popovic V, Damjanovic S, Micic D, Djurovic M, Dieguez C, Casanueva FF (1995) Blocked growth hormone-releasing peptide (GHRP-6)-induced GH secretion and absence of the synergic action of GHRP-6 plus GH-releasing hormone in patients with hypothalamopituitary disconnection: Evidence that GHRP-6 main action is exerted at the hypothalamic level. J Clin Endocrinol Metab 80:942-947.
9. Popovic V, Miljic D, Micic D, Damjanovic S, Arvat E, et al (2003) Ghrelin main action on the regulation of growth hormone release is exerted at hypothalamic level. J Clin Endocrinol Metab 88:3450-3453.
10. Pombo M, Barreiro J, Peñalva A, Peino R, Dieguez C, Casanueva FF (1995) Absence of growth hormone (GH) secretion after the administration of either GH-releasing hormone (GHRH), GH-releasing peptide (GHRP-6), or GHRH plus GHRP-6 in children with neonatal pituitary stalk transection. J Clin Endocrinol Metab 80:3180-3184.
11. Pandya N, DeMott-Friberg R, Bowers CY, Barkan AL, Jaffe CA (1998) Growth hormone (GH)-releasing peptide-6 requires endogenous hypothalamic GH-releasing hormone for maximal GH stimulation. J Clin Endocrinol Metab 83:1186-1189.
12. Guillaume V, Magnan E, Cataldi M, Dutour A, Sauze N, et al (1994) Growth hormone (GH)-releasing hormone secretion is stimulated by a new GH-releasing hexapeptide in sheep. Endocrinology 135:1073-1076.
13. Maheshwari HG, Rahim A, Shalet SM, Baumann G (1999) Selective lack of growth hormone (GH) response to the GH-releasing peptide hexarelin in patients with GH-releasing hormone receptor deficiency. J Clin Endocrinol Metab 84:956-959.
14. 2 on growth hormone (GH)-releasing factor-stimulated GH release and intracellular adenosine 3′,5′-monophosphate accumulation in rat primary pituitary cell culture. Endocrinology 124:2791-1798.
15. 2-induced growth hormone release from rat primary pituitary cells. Endocrinology 129:3337-3342.
16. Cheng K, Chan WW, Butler B, Wei L, Schoen WR, et al (1993) Stimulation of growth hormone elease from rat primary pituitary cells by L-692-429, a novel non-peptidyl GH secretagogue. Endocrinology 132:2729-2731.
17. Cunha SR, Mayo KE (2002) Ghrelin and growth hormone (GH) secretagogues potentiate GH-releasing hormone (GHRH)-induced cyclic adenosine 3′, 5′-monophosphate production in cells expressing transfected GHRH and GH secretagogue receptors. Endocrinology 143:4570-4572.
18. Kineman RD, Luque RM (2007) Evidence that ghrelin is as potent as growth hormone (GH)-releasing hormone (GHRH) in releasing GH from primary pituitary cell cultures of a nonhuman primate (Papio anubis), acting through intracellular signaling pathways distinct from GHRH. Endocrinology 148:4440-4449.
19. Rekasi Z, Czompoly T, Schally AV, Halmos G (2000) Isolation and sequencing of cDNAs for splice variants of growth hormone-releasing hormone receptors from human cancers. Proc Natl Acad Sci USA 97:10561-10566.
20. Pinski J, Izdebski J, Jungwirth A, Groot K, Schally AV (1996) Effect of chronic administration of a new potent agonist of GH-RH(1-29)NH2 on linear growth and GH responsiveness in rats. Regul Pept 65:197-201.
21. Rekasi Z, Varga JL, Schally AV, Halmos G, Armatis P, et al (2000) Antagonists of growth hormone-releasing hormone and vasoactive intestinal peptide inhibit tumor proliferation by different mechanisms: Evidence from in vitro studies on human prostatic and pancreatic cancers. Endocrinology 141:2120-2128.
22. Carreira MC, Camiña JP, Díaz-Rodríguez E, Alvear-Perez R, Llorens-Cortes C, Casanueva FF (2006) Adenosine does not bind to the growth hormone secretagogue receptor type-1a (GHS-R1a). J Endocrinol 191:147-157.
23. Rekasi Z, Varga JL, Schally AV, Halmos G, Groot K, Czompoly T (2000) Antagonistic actions of analogs related to growth hormone-releasing hormone (GHRH) on receptors for GHRH and vasoactive intestinal peptide on rat pituitary and pineal cells in vitro. Proc Natl Acad Sci USA 97:1218-1223.
24. Robberecht P, Coy DH, Waelbroeck M, Heiman ML, de Neef P, et al (1985) Structural requirements for the activation of rat anterior pituitary adenylate cyclase by growth hormone-releasing factor (GRF): Discovery of (N-Ac-Tyr1, D-Arg2)-GRF(1-29)-NH2 as a GRF antagonist on membranes. Endocrinology 117:1759-1764.
25. Buchholz S, Schally AV, Engel JB, Hohla F, Heinrich E, et al (2007) Potentiation of mammary cancer inhibition by combination of antagonists of growth hormone-releasing hormone with docetaxel. Proc Natl Acad Sci USA 104:1943-1946.
26. Schally AV, Varga JL, Engel JB (2008) Antagonists of growth-hormone- releasing hormone: An emerging new therapy for cancer. Nat Clin Pract Endocrinol Metab 4:33-43.
27. Camina JP, Carreira MC, El Messari S, Llorens-Cortes C, Smith RG, Casanueva FF (2004) Desensitization and endocytosis mechanisms of ghrelin-activated growth hormone secretagogue receptor 1a. Endocrinology 145:930-940.
28. Springael JY, Urizar E, Costagliola S, Vassart G, Parmentier M (2007) Allosteric properties of G protein-coupled receptor oligomers. Pharmacol Ther 115:410-418.
29. Schwartz TW, Holst B (2007) Allosteric enhancers, allosteric agonists and ago-allosteric modulators: Where do they bind and how do they act? Trends Pharmacol Sci 28:366-373.
30. Binet V, Brajon C, Le Corre L, Acher F, Pin JP, Prézeau L (2004) The heptahelical domain of GABA(B2) is activated directly by CGP7930, a positive allosteric modulator of the GABA(B) receptor. J Biol Chem 279:29085-29091.
31. Holst B, Elling CE, Schwartz TW (2002) Metal ion-mediated agonism and agonist enhancement in melanocortin MC1 and MC4 receptors. J Biol Chem 277:47662-47670.
32. Holst B, Brandt E, Bach A, Heding A, Schwartz TW (2005) Nonpeptide and peptide growth hormone secretagogues act both as ghrelin receptor agonist and as positive or negative allosteric modulators of ghrelin signaling. Mol Endocrinol 19:2400-2411.
33. Varga JL, Schally AV, Csernus VJ, Zarándi M, Halmos G, et al (1999) Synthesis and biological evaluation of antagonists of growth hormone-releasing hormone with high and protracted in vivo activities. Proc Natl Acad Sci USA 96:692-697.
34. Schally AV, Varga JL (2006) Antagonists of growth hormone-releasing hormone in oncology. Comb Chem High Throughput Screen 9:163-170.
35. Varga JL, Schally AV (2006). Handbook of Biologically Active Peptides, ed Kastin A. (Elsevier-Academic, New York), pp. 483-489.
36. Izdebski J, Pinski J, Horvath JE, Halmos G, Groot K, Schally AV (1995) Synthesis and biological evaluation of superactive agonists of growth hormone-releasing hormone. Proc Natl Acad Sci USA 92:4872-4876.
37. Pazos Y, Alvarez CJP, Camiña JP, Casanueva FF (2007) Stimulation of extracellular signal-regulated kinases and proliferation in the human gastric cancer cells KATO-III by obestatin. Growth Factors 25:373-381.
38. Camiña JP, Casabiell X, Casanueva FF (1999) Inositol 1,4,5-trisphosphate-independent Ca(2+)mobilization triggered by a lipid factor isolated from vitreous body. J Biol Chem 274:28134-28141.