AntiobesityResearch.comA Researcher's Resource for Obesity Therapeutics Growth Hormone System |
MOLECULAR TARGETS
| Molecule | Obesity/IR? | Remarks [references] |
| Growth Hormone | Decrease | [1,5,6,11] |
| Ghrelin | Increase | [2-4,6-14] |
| GOAT | Increase | [3,4] |
COMMERCIAL: LEADS --> PRODUCTS
| Target | Compound | Company [references] |
| GHR | AOD-9640 | Metabolic [1,5,6,11] |
| GHSR | NOX-B11 | N/K [3,8] |
| GHSR | TZP-301 | Tranzyme [11] |
| GHSR | EX-1305 | Elixir [11] |
| GHSR | CYT-009 | Cytos [11] |
| GOAT | N/K | N/K [3] |
Abbreviations: GHR=growth hormone receptor; GHSR=growth hormone secretogogue receptor; GOAT=ghrelin O-acyltransferase; N/K=not known
References
|
1. Aronne LJ,
Thornton-Jones ZD. New targets for obesity
pharmacotherapy. Clin
Pharmacol Ther. 2007 May;81(5):748-52. 2. Dimaraki EV, Jaffe
CA. Role of endogenous ghrelin in growth
hormone secretion, appetite regulation and metabolism. Rev
Endocr Metab Disord. 2006 Dec;7(4):237-49. 3. Gualillo O, Lago F,
Dieguez C. Introducing GOAT: a target for obesity
and anti-diabetic drugs? Trends
Pharmacol Sci. 2008 Aug;29(8):398-401. 4. Gauna C, van de Zande
B, van Kerkwijk A, Themmen AP, van der Lely AJ, Delhanty PJ. Unacylated ghrelin is not a functional
antagonist but a full agonist of the type 1a growth hormone secretagogue
receptor (GHS-R). Mol Cell
Endocrinol. 2007 Aug 15;274(1-2):30-4. 5. Heal DJ, Smith SL,
Fisas A, Codony X, Buschmann H. Selective 5-HT6 receptor ligands:
progress in the development of a novel pharmacological approach to the
treatment of obesity and related metabolic disorders. Pharmacol Ther. 2008 Feb;117(2):207-31. 6. Hofbauer KG,
Nicholson JR, Boss O. The obesity epidemic: current and
future pharmacological treatments. Annu Rev Pharmacol Toxicol. 2007;47:565-92. 7. Kola B, Farkas I,
Christ-Crain M, Wittmann G, Lolli F, Amin F, Harvey-White J, Liposits Z, Kunos
G, Grossman AB, Fekete C, Korbonits M. The orexigenic effect of ghrelin is
mediated through central activation of the endogenous cannabinoid system. PLoS ONE. 2008 Mar 12;3(3):e1797. 8. Zigman JM, Elmquist
JK. In search of an effective obesity
treatment: a shot in the dark or a shot in the arm? Proc Natl Acad Sci U S A. 2006 Aug 29;103(35):12961-2. 9. Bennett NR, Boyne MS,
Cooper RS, Royal-Thomas TY, Bennett FI, Luke A, Wilks RJ, The impact of adiponectin and ghrelin
on incident glucose intolerance and on weight change. Clin Endocrinol (Oxf). 2008;70:408-414. 10. Wilding J. AOD-9604 Metabolic. Curr Opin Investig Drugs. 2004;5(4):436-40. 11. Depoortere I. Targeting the ghrelin receptor to regulate food intake. Regul Pept. 2009 Apr 10. 12. Huda MS, Dovey T,
Wong SP, English PJ, et al. Ghrelin restores 'lean-type' hunger and
energy expenditure profiles in morbidly obese subjects but has no effect on
postgastrectomy subjects. Int
J Obes (Lond). 2009 Mar;33(3):317-25. 13. Li H, Anderes KL,
Kraynov EA, Luthin DR, Do QQ, Hong Y, Tompkins E, et al. Discovery of a novel, orally active,
small molecule gonadotropin-releasing hormone (GnRH) receptor antagonist. J Med Chem. 2006 Jun 1;49(11):3362-7. Erratum in: J
Med Chem. 2006 Sep 21;49(19):5849. 14. Rudolph J, Esler WP,
O'connor S, Coish PD, Wickens PL, Brands M, et al. Quinazolinone derivatives as orally
available ghrelin receptor antagonists for the treatment of diabetes and
obesity. J Med Chem. 2007 Oct
18;50(21):5202-16. |