Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDC00127

Target Information
NameGrowth hormone secretagogue receptor type 1    
Type of targetClinical trial target    
SynonymsGH-releasing peptide receptor    
GHRP    
GHS-R    
Ghrelin receptor    
Growth hormone secretagogue receptor    
DiseaseAnorexia
[ICD9: 307.1   ICD10: F50.0-F50.1]
[1][2][3]
Cachexia
[ICD9: 799.4   ICD10: R64]
[1][3]
Cardiovascular disease, unspecified
[ICD9: 390-459   ICD10: I00-I99]
[4]
Gastrointestinal Diseases and Disorders, miscellaneous[5][6][7]
Gastroparesis
[ICD9: 536.3   ICD10: K31.8]
[5][6][7]
Ileus
[ICD9: 537.2, 560.1, 560.31, 777.1, 777.4   ICD10: K31.5, K56.0, K56.3, K56.7, P76.1]
[5][6][7]
Noninsulin-dependent diabetes mellitus
[ICD9: 250   ICD10: E08-E13]
[2]
Drug(s)TZP-101Phase IIbIleus, Gastroparesis, Miscellaneous Gastrointestinal Disorders[5][6][7]
AnamorelinPhase IICachexia, Anorexia[1]
SUN-11031Phase IIAnorexia nervosa Cachexia[8]
CYT-009-GhrQbDiscontinued in Phase I/IIObesity[9]
AEZS-123PreclinicalAlcohol dependence[10]
EP-01492PreclinicalObesity[9]
TZP-301PreclinicalMetabolic disorders[11]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
PathwayNeuroactive ligand-receptor interaction
UniProt IDQ92847
FunctionReceptor for ghrelin, coupled to g-alpha-11 proteins. Stimulates growth hormone secretion. Binds also other growth hormone releasing peptides (ghrp) (e.g. Met-enkephalin and ghrp-6) as well as non-peptide, low molecular weight secretagogues.    
SequenceMWNATPSEEPGFNLTLADLDWDASPGNDSLGDELLQLFPAPLLAGVTATCVALFVVGIAG NLLTMLVVSRFRELRTTTNLYLSSMAFSDLLIFLCMPLDLVRLWQYRPWNFGDLLCKLFQ FVSESCTYATVLTITALSVERYFAICFPLRAKVVVTKGRVKLVIFVIWAVAFCSAGPIFV LVGVEHENGTDPWDTNECRPTEFAVRSGLLTVMVWVSSIFFFLPVFCLTVLYSLIGRKLW RRRRGDAVVGASLRDQNHKQTVKMLAVVVFAFILCWLPFHVGRYLFSKSFEPGSLEIAQI SQYCNLVSFVLFYLSAAINPILYNIMSKKYRVAVFRLLGFEPFSQRKLSTLKDESSRAWT ESSINT
Target ValidationClick to Find Target Validation Information.    
Inhibitor4- (3-hexylureido)-N-phenylbenzenesulfonamide[12]
AwFwLL-NH2[13]
CP-424391-18[14]
DprwFwLL-NH2[13]
DwFwLL-NH2[13]
GHRELIN[15]
HwFwLL-NH2[13]
KwFwLL-NH2[13]
QwFwLL-NH2[13]
RwFwLL-NH2[13]
rPKPfQwFwLL-NH2[13]
wFwGG-NH2[13]
wFwLL-NH2[13]
AgonistGHRP-2[3]
SUN-11031[8]
TZP-101[5][6][7]
AntagonistAEZS-123[10]
CYT-009-GhrQb[9]
EP-01492[9]
TZP-301[11]
StimulatorAnamorelin[1]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Pharmacodynamic hormonal effects of anamorelin, a novel oral ghrelin mimetic and growth hormone secretagogue in healthy volunteers. Growth Horm IGF Res. 2009 Jun;19(3):267-73. Epub 2009 Feb 3. To Reference
Ref 2Antagonism of ghrelin receptor reduces food intake and body weight gain in mice. Gut. 2003 Jul;52(7):947-52. To Reference
Ref 3GH-releasing peptide-2 increases fat mass in mice lacking NPY: indication for a crucial mediating role of hypothalamic agouti-related protein. Endocrinology. 2002 Feb;143(2):558-68. To Reference
Ref 4[125I-His(9)]-ghrelin, a novel radioligand for localizing GHS orphan receptors in human and rat tissue: up-regulation of receptors with athersclerosis. Br J Pharmacol. 2001 Sep;134(1):143-9. To Reference
Ref 5Contribution of protein binding to the pharmacokinetics of the ghrelin receptor agonist TZP-101 in healthy volunteers and adults with symptomatic gastroparesis: two randomized, double-blind studies and a binding profile study. Clin Drug Investig. 2009;29(6):409-18. doi: 10.2165/00044011-200929060-00004. To Reference
Ref 6Ghrelin receptor agonist (TZP-101) accelerates gastric emptying in adults with diabetes and symptomatic gastroparesis. Aliment Pharmacol Ther. 2009 Jun 1;29(11):1179-87. Epub 2009 Feb 27. To Reference
Ref 7Eur J Pharmacol. 2009 Feb 14;604(1-3):132-7. Epub 2008 Dec 14.Effect of the ghrelin receptor agonist TZP-101 on colonic transit in a rat model of postoperative ileus. To Reference
Ref 8Emerging drugs for eating disorder treatment. Expert Opin Emerg Drugs. 2006 May;11(2):315-36. To Reference
Ref 9Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60. To Reference
Ref 102011 Pipeline of Aeterna Zentaris. To Reference
Ref 112011 Pipeline of Tranzyme Pharma. To Reference
Ref 12Bioorg Med Chem Lett. 2009 Nov 1;19(21):6237-40. Epub 2009 Aug 26.Discovery and optimization of novel 4-[(aminocarbonyl)amino]-N-[4-(2-aminoethyl)phenyl]benzenesulfonamide ghrelin receptor antagonists. To Reference
Ref 13J Biol Chem. 2007 May 25;282(21):15799-811. Epub 2007 Mar 19.Identification of an efficacy switch region in the ghrelin receptor responsible for interchange between agonism and inverse agonism. To Reference
Ref 14Bioorg Med Chem Lett. 2000 Jan 3;10(1):5-8.Modeling directed design and biological evaluation of quinazolinones as non-peptidic growth hormone secretagogues. To Reference
Ref 15J Med Chem. 2009 Apr 23;52(8):2196-203.Fluorine and rhenium substituted ghrelin analogues as potential imaging probes for the growth hormone secretagogue receptor. To Reference



 

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