Insights from growth hormone receptor blockade

Current Opinion in Investigational Drugs

Volumn 5, Issue 10, 2004, Pages 1072-1079

  Muller, Alex F ^a   Van Der Lely, Aart Jan ^b  

^a DEPARTMENT OF SURGERY   (Netherlands)

^b ERASMUS MEDICAL CENTER   (Netherlands)

Author keywords

Body composition; Fasting; Ghrelin; Growth hormone Deficiency; Growth hormone receptor; Growth hormone releasing peptide; Growth hormone secretagogue; Pegvisomant

Indexed keywords

DRUG DERIVATIVE; GROWTH HORMONE; GROWTH HORMONE RECEPTOR; HUMAN GROWTH HORMONE; PEGVISOMANT;

ACROMEGALY; ANIMAL; DIET RESTRICTION; DRUG ANTAGONISM; HUMAN; METABOLISM; REVIEW; SECRETION;

ACROMEGALY; ANIMALS; FASTING; GROWTH HORMONE; HUMAN GROWTH HORMONE; HUMANS; RECEPTORS, SOMATOTROPIN;

EID: 16644361950     PISSN: 14724472     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Review

References (73)

1. Goffin V, Touraine P: Pegvisomant. Pharmacia. Curr Opin Investig Drugs (2002) 3(5):752-757.
2. Kopchick JJ, Parkinson C, Stevens EC, Trainer PJ: Growth hormone receptor antagonists: Discovery, development, and use in patients with acromegaly. Endocr Rev (2002) 23(5):623-646.
3. van der Lely AJ, de Herder WW, Lamberts SW: New medical treatment for acromegaly. Pituitary (1999) 2(1):89-92.
4. de Vos AM, Ultsch M, Kossiakoff AA: Human growth hormone and extracellular domain of its receptor: Crystal structure of the complex. Science (1992) 255(5042):306-312.
5. Cunningham BC, Ultsch M, de Vos AM, Mulkerrin MG, Clauser KR, Wells JA: Dimerization of the extracellular domain of the human growth hormone receptor by a single hormone molecule. Science (1991) 254(5033):821- 825.
6. Ultsch M, de Vos AM, Kossiakoff AA: Crystals of the complex between human growth hormone and the extracellular domain of its receptor. J Mol Biol (1991) 222(4):865-868.
7. Chen WY, Chen NY, Yun J, Wight DC, Wang XZ, Wagner TE, Kopchick JJ: Amino acid residues in the third α-helix of growth hormone involved in growth promoting activity. Mol Endocrinol (1995) 9(3):292-302.
8. Chen WY, Wight DC, Wagner TE, Kopchick JJ: Expression of a mutated bovine growth hormone gene suppresses growth of transgenic mice. Proc Natl Acad Sci USA (1990) 87(13):5061-5065.
9. Fuh G, Cunningham BC, Fukunaga R, Nagata S, Goeddel DV, Wells JA: Rational design of potent antagonists to the human growth hormone receptor. Science (1992) 256(5064):1677-1680.
10. Trainer PJ, Drake WM, Katznelson L, Freda PU, Herman-Bonert V, van der Lely AJ, Dimaraki EV, Stewart PM, Friend KE, Vance ML, Besser GM et al: Treatment of acromegaly with the growth hormone-receptor antagonist pegvisomant. N Engl J Med (2000) 342(16):1171-1177.
11. Bertherat J, Bluet-Pajot MT, Epelbaum J: Neuroendocrine regulation of growth hormone. Eur J Endocrinol (1995) 132(1):12-24.
12. Frohman LA, Downs TR, Chomczynski P: Regulation of growth hormone secretion. Front Neuroendocrinol (1992) 13(4):344-405.
13. Giustina A, Veldhuis JD: Pathophysiology of the neuroregulation of growth hormone secretion in experimental animals and the human. Endocr Rev (1998) 19(6):717-797.
14. Le Roith D, Bondy C, Yakar S, Liu JL, Butler A: The somatomedin hypothesis: 2001. Endocr Rev (2001) 22(1):53-74.
15. Tannenbaum GS, Guyda HJ, Posner BI: Insulin-like growth factors: A role in growth hormone negative feedback and body weight regulation via brain. Science (1983) 220(4592):77-79.
16. Harel Z, Tannenbaum GS: Centrally administered insulin-like growth factor II fails to alter pulsatile growth hormone secretion or food intake. Neuroendocrinology (1992) 56(2):161-168.
17. 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):656-660.
18. Kojima M, Hosoda H, Matsuo H, Kangawa K: Ghrelin: Discovery of the natural endogenous ligand for the growth hormone secretagogue receptor. Trends Endocrinol Metab (2001) 12(3):118-122.
19. Bowers CY, Momany FA, Reynolds GA, Hong A: On the in vitro and in vivo activity of a new synthetic hexapeptide that acts on the pituitary to specifically release growth hormone. Endocrinology (1984) 114(5):1537-1545.
20. Ghigo E, Arvat E, Muccioli G, Camanni F: Growth hormone-releasing peptides. Eur J Endocrinol (1997) 136(5):445-460.
21. Momany FA, Bowers CY, Reynolds GA, Hong A, Newlander K: Conformational energy studies and in vitro and in vivo activity data on growth hormone-releasing peptides. Endocrinology (1984) 114(5):1531-1536.
22. Casanueva FF, Dieguez C: Growth hormone secretagogues: Physiological role and clinical utility. Trends Endocrinol Metab (1999) 10(1):30-38.
23. Smith RG, Van der Ploeg LH, Howard AD, Feighner SD, Cheng K, Hickey GJ, Wyvratt MJ Jr, Fisher MH, Nargund RP, Patchett AA: Peptidomimetic regulation of growth hormone secretion. Endocr Rev (1997) 18(5):621-645.
24. Seoane LM, Tovar S, Baldelli R, Arvat E, Ghigo E, Casanueva FF, Dieguez C: Ghrelin elicits a marked stimulatory effect on GH secretion in freely-moving rats. Eur J Endocrinol (2000) 143(5):R7-R9.
25. Takaya K, Ariyasu H, Kanamoto N, Iwakura H, Yoshimoto A, Harada M, Mori K, Komatsu Y, Usui T, Shimatsu A, Ogawa Y et al: Ghrelin strongly stimulates growth hormone release in humans. J Clin Endocrinol Metab (2000) 85(12):4908-4911.
26. Nagaya N, Kojima M, Uematsu M, Yamagishi M, Hosoda H, Oya H, Hayashi Y, Kangawa K: Hemodynamic and hormonal effects of human ghrelin in healthy volunteers. Am J Physiol Regul Integr Comp Physiol (2001) 280(5):R1483-R1487.
27. Arvat E, Di Vito L, Broglio F, Papotti M, Muccioli G, Dieguez C, Casanueva FF, Deghenghi R, Camanni F, Ghigo E: Preliminary evidence that ghrelin, the natural GH secretagogue (GHS)-receptor ligand, strongly stimulates GH secretion in humans. J Endocrinol Invest (2000) 23(8):493-495.
28. Arvat E, Maccario M, Di Vito L, Broglio F, Benso A, Gottero C, Papotti M, Muccioli G, Dieguez C, Casanueva FF, Deghenghi R et al: Endocrine activities of ghrelin, a natural growth hormone secretagogue (GHS), in humans: Comparison and interactions with hexarelin, a nonnatural peptidyl GHS, and GH-releasing hormone. J Clin Endocrinol Metab (2001) 86(3):1169-1174.
29. Peino R, Baldelli R, Rodriguez-Garcia J, Rodriguez-Segade S, Kojima M, Kangawa K, Arvat E, Ghigo E, Dieguez C, Casanueva FF: Ghrelin-induced growth hormone secretion in humans. Eur J Endocrinol (2000) 143(6):R11-R14.
30. Tschöp M, Smiley DL, Heiman ML: Ghrelin induces adiposity in rodents. Nature (2000) 407(6806):908-913.
31. Wren AM, Small CJ, Ward HL, Murphy KG, Dakin CL, Taheri S, Kennedy AR, Roberts GH, Morgan DG, Ghatei MA, Bloom SR: The novel hypothalamic peptide ghrelin stimulates food intake and growth hormone secretion. Endocrinology (2000) 141(11):4325-4328.
32. Kamegai J, Tamura H, Shimizu T, Ishii S, Sugihara H, Wakabayashi I: Central effect of ghrelin, an endogenous growth hormone secretagogue, on hypothalamic peptide gene expression. Endocrinology (2000) 141(12):4797-4800.
33. Masuda Y, Tanaka T, Inomata N, Ohnuma N, Tanaka S, Itoh Z, Hosoda H, Kojima M, Kangawa K: Ghrelin stimulates gastric acid secretion and motility in rats. Biochem Biophys Res Commun (2000) 276(3):905-908.
34. 1 receptor pathway. Diabetes (2001) 50(2):227-232.
35. Date Y, Nakazato M, Murakami N, Kojima M, Kangawa K, Matsukura S: Ghrelin acts in the central nervous system to stimulate gastric acid secretion. Biochem Biophys Res Commun (2001) 280(3):904-907.
36. Asakawa A, Inui A, Kaga T, Yuzuriha H, Nagata T, Ueno N, Makino S, Fujimiya M, Niijima A, Fujino MA, Kasuga M: Ghrelin is an appetite-stimulatory signal from stomach with structural resemblance to motilin. Gastroenterology (2001) 120(2):337-345.
37. Nakazato M, Murakami N, Date Y, Kojima M, Matsuo H, Kangawa K, Matsukura S: A role for ghrelin in the central regulation of feeding. Nature (2001) 409(6817):194-198.
38. Muller AF, Janssen JA, Hofland LJ, Lamberts SW, Bidlingmaier M, Strasburger CJ, van der Lely AJ: Blockade of the growth hormone (GH) receptor unmasks rapid GH-releasing peptide-6-mediated tissue-specific insulin resistance. J Clin Endocrinol Metab (2001) 86(2):590-593.
39. Muller AF, Leebeek FW, Janssen JA, Lamberts SW, Hofland L, van der Lely AJ: Acute effect of pegvisomant on cardiovascular risk markers in healthy men: Implications for the pathogenesis of atherosclerosis in GH deficiency. J Clin Endocrinol Metab (2001) 86(11):5165-5171.
40. Muller AF, Janssen JA, Lamberts SW, Bidlingmaier M, Strasburger CJ, Hofland L, van der Lely AJ: Effects of fasting and pegvisomant on the GH-releasing hormone and GH-releasing peptide-6 stimulated growth hormone secretion. Clin Endocrinol (2001) 55(4):461-467.
41. Muller AF, Lamberts SW, Janssen JA, Hofland LJ, Koetsveld PV, Bidlingmaier M, Strasburger CJ, Ghigo E, van der Lely AJ: Ghrelin drives GH secretion during fasting in man. Eur J Endocrinol (2002) 146(2):203-207.
42. Ho KY, Veldhuis JD, Johnson ML, Furlanetto R, Evans WS, Alberti KG, Thorner MO: Fasting enhances growth hormone secretion and amplifies the complex rhythms of growth hormone secretion in man. J Clin Invest (1988) 81(4):968-975.
43. Chapman IM, Hartman ML, Pieper KS, Skiles EH, Pezzoli SS, Hintz RL, Thorner MO: Recovery of growth hormone release from suppression by exogenous insulin-like growth factor I (IGF-I): Evidence for a suppressive action of free rather than bound IGF-I. J Clin Endocrinol Metab (1998) 83(8):2836-2842.
44. Frystyk J, Hojlund K, Christensen M, Beck-Nielsen H, Orskov H: Three days of fasting reduces circulating free but not total IGF-I: A possible role for circulating free IGF in the feedback regulation of GH. Growth Horm IGF Res (2000) 10:147.
45. Grundy SM: Hypertriglyceridemia, insulin resistance, and the metabolic syndrome. Am J Cardiol (1999) 83(9B):25F-29F.
46. Haffner SM, Valdez RA, Hazuda HP, Mitchell BD, Morales PA, Stern MP: Prospective analysis of the insulin-resistance syndrome (syndrome X). Diabetes (1992) 41(6):715-722.
47. Landsberg L: Insulin-mediated sympathetic stimulation: Role in the pathogenesis of obesity-related hypertension (or, how insulin affects blood pressure, and why). J Hypertens (2001) 19(3 Pt 2):523-528.
48. Reaven GM: Role of insulin resistance in human disease (syndrome X): An expanded definition. Annu Rev Med (1993) 44:121-131.
49. Vague P, Raccah D: The syndrome of insulin resistance. Horm Res (1992) 38(1-2):28-32.
50. Coon PJ, Rogus EM, Drinkwater D, Muller DC, Goldberg AP: Role of body fat distribution in the decline in insulin sensitivity and glucose tolerance with age. J Clin Endocrinol Metab (1992) 75(4):1125-1132.
51. Ferrannini E, Vichi S, Beck-Nielsen H, Laakso M, Paolisso G, Smith U: Insulin action and age. European Group for the Study of Insulin Resistance (EGIR). Diabetes (1996) 45(7):947-953.
52. Paolisso G, Rizzo MR, Mazziotti G, Tagliamonte MR, Gambardella A, Rotondi M, Carella C, Giugliano D, Varricchio M, D'Onofrio F: Advancing age and insulin resistance: Role of plasma tumor necrosis factor-α. Am J Physiol (1998) 275(2 Pt 1):E294-E299.
53. Paolisso G, Tagliamonte MR, Rizzo MR, Giugliano D: Advancing age and insulin resistance: New facts about an ancient history. Eur J Clin Invest (1999) 29(9):758-769.
54. Shimokata H, Muller DC, Fleg JL, Sorkin J, Ziemba AW, Andres R: Age as independent determinant of glucose tolerance. Diabetes (1991) 40(1):44-51.
55. Chapman IM, Bach MA, Van Cauter E, Farmer M, Krupa D, Taylor AM, Schilling LM, Cole KY, Skiles EH, Pezzoli SS, Hartman ML et al: Stimulation of the growth hormone (GH)-insulin-like growth factor I axis by daily oral administration of a GH secretogogue (MK-677) in healthy elderly subjects. J Clin Endocrinol Metab (1996) 81(12):4249-4257.
56. Murphy MG, Plunkett LM, Gertz BJ, He W, Wittreich J, Polvino WM, Clemmons DR: MK-677, an orally active growth hormone secretagogue, reverses diet-induced catabolism. J Clin Endocrinol Metab (1998) 83(2):320-325.
57. Svensson J, Carlsson B, Carlsson LM, Jansson JO, Bengtsson BA: Discrepancy between serum leptin values and total body fat in response to the oral growth hormone secretagogue MK-677. Clin Endocrinol (1999) 50(4):451-456.
58. Svensson J, Lonn L, Jansson JO, Murphy G, Wyss D, Krupa D, Cerchio K, Polvino W, Gertz B, Boseaus I, Sjostrom L, Bengtsson BA: Two-month treatment of obese subjects with the oral growth hormone (GH) secretagogue MK-677 increases GH secretion, fat-free mass, and energy expenditure. J Clin Endocrinol Metab (1998) 83(2):362-369.
59. Bennett PA, Thomas GB, Howard AD, Feighner SD, Van der Ploeg LH, Smith RG, Robinson IC: Hypothalamic growth hormone secretagogue-receptor (GHS-R) expression is regulated by growth hormone in the rat. Endocrinology (1997) 138(11):4552-4557.
60. Pellegrini E, Carmignac DF, Bluet-Pajot MT, Mounier F, Bennett P, Epelbaum J, Robinson IC: Intrahypothalamic growth hormone feedback: From dwarfism to acromegaly in the rat. Endocrinology (1997) 138(11):4543-4551.
61. Jap TS, Ho LT: Insulin secretion and sensitivity in acromegaly. Clin Physiol Biochem (1990) 8(2):64-69.
62. Unal A, Sahin Y, Kelestimur F: Acromegaly with polycystic ovaries, hyperandrogenism, hirsutism, insulin resistance and acanthosis nigricans: A case report. Endocrine J (1993) 40(2):207-211.
63. Wasada T, Aoki K, Sato A, Katsumori K, Muto K, Tomonaga O, Yokoyama H, Iwasaki N, Babazono T, Takahashi C, Iwamoto Y et al: Assessment of insulin resistance in acromegaly associated with diabetes mellitus before and after transsphenoidal adenomectomy. Endocrine J (1997) 44(4):617-620.
64. Thomas GB, Cummins JT, Francis H, Sudbury AW, McCloud PI, Clarke IJ: Effect of restricted feeding on the relationship between hypophysial portal concentrations of growth hormone (GH)-releasing factor and somatostatin, and jugular concentrations of GH in ovariectomized ewes. Endocrinology (1991) 128(2):1151-1158.
65. Aimaretti G, Colao A, Corneli G, Pivonello R, Maccario M, Morrison K, Pflaum CD, Strasburger CJ, Lombardi G, Ghigo E: The study of spontaneous GH secretion after 36-h fasting distinguishes between GH-deficient and normal adults. Clin Endocrinol (1999) 51(6):771-777.
66. Flavell DM, Wells T, Wells SE, Carmignac DF, Thomas GB, Robinson IC: Dominant dwarfism in transgenic rats by targeting human growth hormone (GH) expression to hypothalamic GH-releasing factor neurons. EMBO J (1996) 15(15):3871-3879.
67. Wells T, Flavell DM, Wells SE, Carmignac DF, Robinson IC: Effects of growth hormone secretagogues in the transgenic growth-retarded (Tgr) rat. Endocrinology (1997) 138(2):580-587.
68. Thorner MO, Strasburger CJ, Wu Z, Straume M, Bidlingmaier M, Pezzoli SS, Zib K, Scarlett JC, Bennett WF: Growth hormone (GH) receptor blockade with a PEG-modified GH (B2036-PEG) lowers serum insulin-like growth factor-I but does not acutely stimulate serum GH. J Clin Endocrinol Metab (1999) 84(6):2098-2103.
69. Popovic V, Damjanovic S, Micic D, Djurovic M, Dieguez C, Casanueva FF: 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 (1995) 80(3):942-947.
70. Pandya N, DeMott-Friberg R, Bowers CY, Barkan AL, Jaffe CA: Growth hormone (GH)-releasing peptide-6 requires endogenous hypothalamic GH-releasing hormone for maximal GH stimulation. J Clin Endocrinol Metab (1998) 83(4):1186-1189.
71. Guillaume V, Magnan E, Cataldi M, Dutour A, Sauze N, Renard M, Razafindraibe H, Conte-Devolx B, Deghenghi R, Lenaerts V: Growth hormone (GH)-releasing hormone secretion is stimulated by a new GH-releasing hexapeptide in sheep. Endocrinology (1994) 135(3):1073-1076.
72. Hartman ML, Veldhuis JD, Johnson ML, Lee MM, Alberti KG, Samojlik E, Thorner MO: Augmented growth hormone (GH) secretory burst frequency and amplitude mediate enhanced GH secretion during a two-day fast in normal men. J Clin Endocrinol Metab (1992) 74(4):757-765.
73. Tschöp M, Weyer C, Tataranni PA, Devanarayan V, Ravussin E, Heiman ML: Circulating ghrelin levels are decreased in human obesity. Diabetes (2001) 50(4):707-709.