Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDS00273

Target Information
NameGonadotropin-releasing hormone receptor    
Type of targetSuccessful target    
SynonymsGnRH receptor    
GnRH-R    
Gonadotrophin releasing hormone receptor    
Hypothalamic gonadotropin-releasing hormone receptor    
DiseaseCancer, unspecific
[ICD9: 140-229   ICD10: C00-C96]
[1]
Hypogonadotropic hypogonadism
[ICD9: 257.2   ICD10: E23.0, E28.3, E29.1]
[2]
Reproductive disorder
[ICD9: 600-629   ICD10: N40-N99]
[3]
Drug(s)CetrorelixApprovedControlled ovarian stimulation[4][5]
GanirelixApprovedRegulates Ovulation[6]
GonadorelinApprovedHypothalamic hypogonadism[7]
Leuprorelin acetateApprovedProstate cancer[8]
NafarelinApprovedEndometriosis[9]
TAK-385Phase IEndometriosis, Uterus myoma[8]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
PathwayGnRH signaling pathway
Neuroactive ligand-receptor interaction
UniProt IDP30968
FunctionReceptor for gonadotropin releasing hormone (gnrh) that mediate the action of gnrh to stimulate the secretion of the gonadotropic hormones (lh and fsh). This receptor mediates its action by association with G proteins that activate a phosphatidylinositol.    
SequenceMANSASPEQNQNHCSAINNSIPLMQGNLPTLTLSGKIRVTVTFFLFLLSATFNASFLLKL QKWTQKKEKGKKLSRMKLLLKHLTLANLLETLIVMPLDGMWNITVQWYAGELLCKVLSYL KLFSMYAPAFMMVVISLDRSLAITRPLALKSNSKVGQSMVGLAWILSSVFAGPQLYIFRM IHLADSSGQTKVFSQCVTHCSFSQWWHQAFYNFFTFSCLFIIPLFIMLICNAKIIFTLTR VLHQDPHELQLNQSKNNIPRARLKTLKMTVAFATSFTVCWTPYYVLGIWYWFDPEMLNRL SDPVNHFFFLFAFLNPCFDPLIYGYFSL
Related US Patent6,172,080
6,180,642
6,214,798
6,288,078
6,346,534
6,384,017
6,537,998
6,540,979
6,569,863
6,583,153
6,608,197
6,620,824
6,627,609
6,673,796
6,677,340
6,765,011
Target ValidationClick to Find Target Validation Information.    
InhibitorACYLINE[10]
AZALINE B[10]
Azaline B derivative[11]
Azaline B derivative[11]
Azaline B derivative[11]
Azaline B derivative[11]
Azaline B derivative[11]
Azaline B derivative[11]
Azaline B derivative[11]
Azaline B derivative[11]
Azaline B derivative[11]
Azaline B derivative[11]
DEGARELIX[12]
DEGARELIX[13]
Degarelix analogue[12]
Degarelix analogue[12]
Degarelix analogue[12]
Degarelix analogue[12]
Degarelix analogue[12]
Degarelix analogue[12]
Degarelix analogue[12]
Degarelix analogue[12]
Degarelix analogue[12]
Degarelix analogue[12]
Degarelix analogue[12]
Degarelix analogue[12]
Degarelix analogue[12]
Degarelix analogue[12]
Degarelix analogue[12]
Degarelix analogue[12]
Degarelix analogue[12]
Degarelix analogue[12]
Degarelix analogue[12]
Degarelix analogue[12]
Degarelix analogue[12]
Degarelix analogue[12]
Degarelix analogue[12]
Degarelix analogue[12]
Degarelix analogue[12]
Degarelix analogue[12]
Degarelix analogue[12]
Degarelix analogue[12]
Degarelix analogue[12]
Degarelix analogue[12]
Degarelix analogue[12]
LEUPRORELIN[14]
LHRH[15]
NBI-42902[16]
T-98475[17]
T-98475[15]
TAK-013[17]
WAY-207024[18]
[4Aph (CO-[13]
[4Aph (CO-NH-[13]
[4Aph (CO-NH-OCH3)5,D-4Aph[13]
[4Aph (CO-NH-OCH3)5]degarelix[13]
[4Aph (CO-NH-OH)5]degarelix[13]
[D-4Aph (CO-NH-[13]
[D-4Aph (CO-NH-OCH3)6]degarelix[13]
[D-4Aph (CO-NH-OH)6]degarelix[13]
[D-Dab (CO-NH-OCH3)3]degarelix[13]
[D-Dab (CO-NH-OH)3]degarelix[13]
[D-Dap (CO-NH-OCH3)3]degarelix[13]
[D-Dap (CO-NH-OH)3]degarelix[13]
[D-Gln3,D-Ncy (SO,isopropyl)7]acyline[10]
[D-Gln3,D-Ncy (SO2,isopropyl)7]acyline[10]
[D-Gln3,D-Ncy (isopropyl)7]acyline[10]
[D-Gln3,Ncy (SO,isopropyl)7]acyline[10]
[D-Gln3,Ncy (SO2,isopropyl)7]acyline[10]
[D-Gln3,Ncy (isopropyl)7]acyline[10]
[D-Ncy (2-naphthyl)1]acyline[10]
[D-Ncy (SO,isopropyl)7]acyline[10]
[D-Ncy (SO,methyl)10]acyline[10]
[D-Ncy (SO,methyl)4]acyline[10]
[D-Ncy (isopropyl)7]acyline[10]
[D-Ncy (methyl)10] acyline[10]
[D-Ncy (methyl)4]acyline[10]
[Ncy (2-naphthyl)1]acyline[10]
[Ncy (SO,isopropyl)7]acyline[10]
[Ncy (SO,methyl)10]acyline[10]
[Ncy (SO,methyl)4]acyline[10]
[Ncy (isopropyl)7]acyline[10]
[Ncy (methyl)10]acyline[10]
[Ncy (methyl)4]acyline[10]
pGlu-His-Trp-Ser-His-D-Tyr-Leu-Arg-Pro-Gly-NH2[19]
pGlu-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly-NH2[19]
AgonistGonadorelin[7]
Leuprorelin acetate[8]
Nafarelin[9]
AntagonistCetrorelix[4][5]
Ganirelix[6]
TAK-385[8]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Intracellular signaling pathways mediated by the gonadotropin-releasing hormone (GnRH) receptor. Arch Med Res. 2001 Nov-Dec;32(6):499-509. To Reference
Ref 2Misrouted cell surface receptors as a novel disease aetiology and potential therapeutic target: the case of hypogonadotropic hypogonadism due to gonadotropin-releasing hormone resistance. Expert Opin Ther Targets. 2003 Apr;7(2):175-85. To Reference
Ref 3Advances in understanding gonadotrophin-releasing hormone receptor structure and ligand interactions. Rev Reprod. 1997 May;2(2):113-20. To Reference
Ref 4Gonadotropin releasing hormone analogs induce apoptosis by extrinsic pathway involving p53 phosphorylation in primary cell cultures of human prostatic adenocarcinomas. Prostate. 2009 Jul 1;69(10):1025-33. To Reference
Ref 5Gonadotrophin-releasing hormone antagonists for assisted conception. Cochrane Database Syst Rev. 2006 Jul 19;3:CD001750. To Reference
Ref 6Age attenuates testosterone secretion driven by amplitude-varying pulses of recombinant human luteinizing hormone during acute gonadotrope inhibition in healthy men. J Clin Endocrinol Metab. 2007 Sep;92(9):3626-32. Epub 2007 Jun 19. To Reference
Ref 7Use of cognitive behavior therapy for functional hypothalamic amenorrhea. Ann N Y Acad Sci. 2006 Dec;1092:114-29. To Reference
Ref 8Takeda. Product Development Pipeline. July 31 2009. To Reference
Ref 9Reversible downregulation of endocrine and germinative testicular function (hormonal castration) in the dog with the GnRH-agonist azagly-nafarelin as a removable implant "Gonazon"; a preclinical trial. Theriogenology. 2009 Apr 15;71(7):1037-45. Epub 2009 Feb 23. To Reference
Ref 10J Med Chem. 2007 May 3;50(9):2067-77. Epub 2007 Apr 3.Structure-activity relationship studies of gonadotropin-releasing hormone antagonists containing S-aryl/alkyl norcysteines and their oxidized derivatives. To Reference
Ref 11Bioorg Med Chem Lett. 2005 Jun 2;15(11):2894-7.Synthesis, in vivo and in vitro biological activity of novel azaline B analogs. To Reference
Ref 12J Med Chem. 2005 Jul 28;48(15):4851-60.Iterative approach to the discovery of novel degarelix analogues: substitutions at positions 3, 7, and 8. Part II. To Reference
Ref 13J Med Chem. 2006 Jun 15;49(12):3536-43.Novel analogues of degarelix incorporating hydroxy-, methoxy-, and pegylated-urea moieties at positions 3, 5, 6 and the N-terminus. Part III. To Reference
Ref 14J Med Chem. 2006 Jun 29;49(13):3809-25.Design, synthesis, and structure-activity relationships of thieno[2,3-b]pyridin-4-one derivatives as a novel class of potent, orally active, non-peptide luteinizing hormone-releasing hormone receptor antagonists. To Reference
Ref 15J Med Chem. 1998 Oct 22;41(22):4190-5.Discovery of a novel, potent, and orally active nonpeptide antagonist of the human luteinizing hormone-releasing hormone (LHRH) receptor. To Reference
Ref 16J Med Chem. 2008 Dec 11;51(23):7478-85.Discovery of sodium R-(+)-4-{2-[5-(2-fluoro-3-methoxyphenyl)-3-(2-fluoro-6-[trifluoromethyl]benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenylethylamino}butyrate (elagolix), a potent and orally available nonpeptide antagonist of the human gonadotropin-releasing hormone receptor. To Reference
Ref 17J Med Chem. 2008 Jun 26;51(12):3331-48.Non-peptide gonadotropin-releasing hormone receptor antagonists. To Reference
Ref 18Bioorg Med Chem Lett. 2010 Apr 15;20(8):2512-5. Epub 2010 Mar 3.Synthesis and biological evaluation of piperazinyl heterocyclic antagonists of the gonadotropin releasing hormone (GnRH) receptor. To Reference
Ref 19J Med Chem. 2006 Jan 26;49(2):637-47.Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. To Reference



 

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