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Version 2.5
Creation Date 2005-06-13 13:24:05
Update Date 2009-02-19 16:03:21
Primary Accession Number DB00050
Secondary Accession Number
  • APRD00686
  • BIOD00115
  • BTD00115
Name Cetrorelix
Drug Type
  • Approved
  • Biotech
  • Investigational
Description Cetrorelix is a man-made hormone that blocks the effects of Gonadotropin Releasing Hormone (GnRH). GnRH controls another hormone that is called luteinizing hormone (LH), which is the hormone that starts ovulation during the menstrual cycle. When undergoing hormone treatment sometimes premature ovulation can occur, leading to eggs that are not ready for fertilization to be released. Cetrorelix does not allow the premature release of these eggs to occur.
Synonyms
  1. Cetrorelix Acetate
  2. Cetrorelixum [INN-Latin]
  3. SB 75
  4. SB-75
Brand Names
  1. Cetrotide
Brand Mixtures Not Available
Chemical IUPAC Name 1-[(2S)-2-[[(2S)-2-[[(2R)-2-[[(2R)-2-[[(2R)-2-[[(2R)-2-[[(2S)-2-[[(2R)-2-acetamido-3-naphthalen-2-ylpropanoyl]amino]-3-(4-chlorophenyl)propanoyl]amino]-3-pyridin-3-ylpropanoyl]amino]-3-hydroxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-5-(carbamoylamino)pentanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]-N-[(2R)-1-amino-1-oxopropan-2-yl]pyrrolidine-2-carboxamide
Chemical Formula C72H96ClN17O16
Chemical Structure Structure
Protein Sequence(s) Not Available
CAS Registry Number 120287-85-6
InChI Identifier InChI=1/C70H92ClN17O14.C2H4O2/c1-39(2)31-52(61(94)82-51(15-9-28-77-69(73)74)68(101)88-30-10-16-58(88)67(100)79-40(3)59(72)92)83-60(93)50(14-8-29-78-70(75)102)81-63(96)54(34-43-20-25-49(91)26-21-43)86-66(99)57(38-89)87-65(98)56(36-45-11-7-27-76-37-45)85-64(97)55(33-42-18-23-48(71)24-19-42)84-62(95)53(80-41(4)90)35-44-17-22-46-12-5-6-13-47(46)32-44;1-2(3)4/h5-7,11-13,17-27,32,37,39-40,50-58,89,91H,8-10,14-16,28-31,33-36,38H2,1-4H3,(H2,72,92)(H,79,100)(H,80,90)(H,81,96)(H,82,94)(H,83,93)(H,84,95)(H,85,97)(H,86,99)(H,87,98)(H4,73,74,77)(H3,75,78,102);1H3,(H,3,4)/t40-,50-,51+,52+,53-,54+,55-,56-,57+,58+;/m1./s1/f/h73,77-87H,72,74-75H2;3H
InChI Key KFEFLCOCAHJBEA-VSMDNYHMDI
KEGG Drug D01685 Link Image
KEGG Compound Not Available
PubChem Compound 16129715 Link Image
PubChem Substance 7848748 Link Image
ChEBI ID Not Available
PharmGKB ID PA10255 Link Image
HET ID Not Available
GenBank ID Not Available
Drug ID Number [DIN] 02247767 Link Image
RxList Link http://www.rxlist.com/cgi/generic2/cetrorelix.htm Link Image
PDRhealth Link Not Available
Wikipedia Link http://en.wikipedia.org/wiki/Cetrorelix Link Image
FDA Label
Material Safety Data Sheet (MSDS) Not Available
Synthesis Reference Not Available
Average Molecular Weight 1491.0900
Monoisotopic Molecular Weight 1489.6909
State Solid
Melting Point Not Available
Experimental Water Solubility Not Available Source: PhysProp
Predicted Water Solubility Not Available Calculated using ALOGPS
Experimental LogP/Hydrophobicity Not Available Source: PhysProp
Predicted LogP Not Available Calculated using ALOGPS
Experimental LogS Not Available
Predicted LogS Not Available Calculated using ALOGPS
Experimental Caco2 Permeability Not Available
pKa/Isoelectric Point Not Available
Mass Spectrum Not Available
MOL File Show Link Image | Download Link Image
SDF File Show Link Image | Download Link Image
PDB File Show Link Image | Download Link Image
2D Structure
3D Structure
Experimental PDB ID Not Available
Isomeric SMILES CC(O)=O.CC(C)C[C@H](NC(=O)[C@@H](CCCNC(N)=O)NC(=O)[C@H](CC1=CC=C(O)C=C1)NC(=O)[C@H](CO)NC(=O)[C@@H](CC1=CC=CN=C1)NC(=O)[C@@H](CC1=CC=C(Cl)C=C1)NC(=O)[C@@H](CC1=CC2=CC=CC=C2C=C1)NC(C)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O
Canonical SMILES CC(O)=O.CC(C)CC(NC(=O)C(CCCNC(N)=O)NC(=O)C(CC1=CC=C(O)C=C1)NC(=O)C(CO)NC(=O)C(CC1=CC=CN=C1)NC(=O)C(CC1=CC=C(Cl)C=C1)NC(=O)C(CC1=CC2=CC=CC=C2C=C1)NC(C)=O)C(=O)NC(CCCNC(N)=N)C(=O)N1CCCC1C(=O)NC(C)C(N)=O
Drug Category
  • Hormone Antagonists
  • Infertility Agents
ATC Codes
AHFS Codes
  • 92:00.00
Indication For the inhibition of premature LH surges in women undergoing controlled ovarian stimulation
Pharmacology Cetrorelix is a synthetic decapeptide with gonadotropin-releasing hormone (GnRH) antagonistic activity. GnRH induces the production and release of luteinizing hormone (LH) and follicle stimulating hormone (FSH) from the gonadotrophic cells of the anterior pituitary. Due to a positive estradiol (E2) feedback at midcycle, GnRH liberation is enhanced resulting in an LH-surge. This LH-surge induces the ovulation of the dominant follicle, resumption of oocyte meiosis and subsequently luteinization as indicated by rising progesterone levels. Cetrorelix competes with natural GnRH for binding to membrane receptors on pituitary cells and thus controls the release of LH and FSH in a dose-dependent manner.
Mechanism of Action Cetrorelix binds to the gonadotropin releasing hormone receptor and acts as a potent inhibitor of gonadotropin secretion. It competes with natural GnRH for binding to membrane receptors on pituitary cells and thus controls the release of LH and FSH in a dose-dependent manner.
Absorption Rapidly absorbed following subcutaneous injection. The mean absolute bioavailability following subcutaneous administration to healthy female subjects is 85%.
Toxicity Not Available
Protein Binding 86%
Biotransformation In in vitro studies, cetrorelix was stable against phase I- and phase II-metabolism. Cetrorelix was transformed by peptidases, and the (1-4) peptide was the predominant metabolite.
Half Life ~62.8 hours
Dosage Forms
Form Route
Powder, for solution Subcutaneous
Powder, for solution Subcutaneous
Powder, for solution Subcutaneous
Patient Information Show Link Image
Contraindications Show Link Image
Interactions Show Link Image
Drug Interactions Not Available
Food Interactions Not Available
Pathways Not Available
General References
  1. Drugs.com Link Image
  2. Wikipedia Link Image
  3. RxList Link Image
Organisms Affected
  • Humans and other mammals
Targets
  1. Lutropin-choriogonadotropic hormone receptor
  2. Gonadotropin-releasing hormone receptor
Drug Target 1 [top]
Target 1 ID 148
Target 1 Name Lutropin-choriogonadotropic hormone receptor
Target 1 Synonyms
  1. LH/CG-R
  2. LHR
  3. LSH- R
  4. Luteinizing hormone receptor
  5. Lutropin-choriogonadotropic hormone receptor precursor
Target 1 Gene Name LHCGR
Target 1 Protein Sequence >Lutropin-choriogonadotropic hormone receptor precursor 
MKQRFSALQLLKLLLLLQPPLPRALREALCPEPCNCVPDGALRCPGPTAGLTRLSLAYLP
VKVIPSQAFRGLNEVIKIEISQIDSLERIEANAFDNLLNLSEILIQNTKNLRYIEPGAFI
NLPRLKYLSICNTGIRKFPDVTKVFSSESNFILEICDNLHITTIPGNAFQGMNNESVTLK
LYGNGFEEVQSHAFNGTTLTSLELKENVHLEKMHNGAFRGATGPKTLDISSTKLQALPSY
GLESIQRLIATSSYSLKKLPSRETFVNLLEATLTYPSHCCAFRNLPTKEQNFSHSISENF
SKQCESTVRKVSNKTLYSSMLAESELSGWDYEYGFCLPKTPRCAPEPDAFNPCEDIMGYD
FLRVLIWLINILAIMGNMTVLFVLLTSRYKLTVPRFLMCNLSFADFCMGLYLLLIASVDS
QTKGQYYNHAIDWQTGSGCSTAGFFTVFASELSVYTLTVITLERWHTITYAIHLDQKLRL
RHAILIMLGGWLFSSLIAMLPLVGVSNYMKVSICFPMDVETTLSQVYILTILILNVVAFF
IICACYIKIYFAVRNPELMATNKDTKIAKKMAILIFTDFTCMAPISFFAISAAFKVPLIT
VTNSKVLLVLFYPINSCANPFLYAIFTKTFQRDFFLLLSKFGCCKRRAELYRRKDFSAYT
SNCKNGFTGSNKPSQSTLKLSTLHCQGTALLDKTRYTEC
Target 1 Number of Residues 710
Target 1 Molecular Weight 78617
Target 1 Theoretical pI 8.58
Target 1 GO Classification
Function
lutropin-choriogonadotropic hormone receptor activity
protein-hormone receptor activity
signal transducer activity
receptor activity
transmembrane receptor activity
G-protein coupled receptor activity
rhodopsin-like receptor activity
Process
cellular process
cell communication
signal transduction
cell surface receptor linked signal transduction
G-protein coupled receptor protein signaling pathway
Component
cell
membrane
intrinsic to membrane
integral to membrane
Target 1 General Function Involved in rhodopsin-like receptor activity
Target 1 Specific Function Receptor for lutropin-choriogonadotropic hormone. The activity of this receptor is mediated by G proteins which activate adenylate cyclase
Target 1 Pathways Not Available
Target 1 Reactions Not Available
Target 1 Pfam Domain Function
Target 1 Signals
  • 1-26
Target 1 Transmembrane Regions
  • 364-385
  • 396-416
  • 440-462
  • 483-505
  • 526-549
  • 571-594
  • 606-627
Target 1 Essentiality Non-Essential
Target 1 GenBank ID Protein 903746 Link Image
Target 1 UniProtKB/Swiss-Prot ID P22888 Link Image
Target 1 UniProtKB/Swiss-Prot Entry Name LSHR_HUMAN Link Image
Target 1 PDB ID Not Available
Target 1 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 1 Gene Sequence >2058 bp 
ATGAAGCAGCGGTTCTCGCCGCTGCAGCTGCTGAAGCTGCTGCTGCTGCTGCAGGCGCCG
CTGCCACGAGCGCTGCGCAGGCTCTGCCCTGAGCCCTGCAACTGCGTGCCCGACGGCGCC
CTGCGTGCCCCGGCCCCACGGCCGTCCACTCGACTATCACTTGCCTACCTCCCTGTCAAA
GTGATCCCATCTCAAAGTTTCAGAGGACTTAATGAGGTCATAAAAATTGAAATCTCTCAG
ATTGATTCCCTGGAAAGGATAGAAGCTAATGCCTTTGACAACCTCCTCAATTTGTCTGAA
ATACTGATCCAGAACACCAAAAATCTGAGATACATTGAGCCCGGAGCATTTATAAATCTT
CCCCGATTAAAATACTTGAGCATCTGTAACACAGGCATCAGAAAGTTTCCAGATGTTACG
AAGGTCTTCTCCTCTGAATCAAATTTCATTCTGGAAATTTGTGATAACTTACACATAACC
ACCATACCAGGAAATGCTTTTCAAGGGATGAATAATGAATCTGTAACACTCAAACTATAT
GGAAATGGATTTGAAGAAGTACAAAGTCATGCATTCAATGGGACGACACTGACTTCACTG
GAGCTAAAGGAAAACGTACATCTGGAGAAGATGCACAATGGAGCCTTCCGTGGGGCCACA
GGGCCGAAAACCTTGGATATTTCTTCCACCAAATTGCAGGCCCTGCCGAGCTATGGCCTA
GAGTCCATTCAGAGGCTAATTGCCACGTCATCCTATTCTCTAAAAAAATTGCCATCAAAA
CAAACATTTGTCAATCTCCTGAGGGCCACGCTTCATTACCCCAGCCACTGCTGTGCATTT
AGAAACTTGCCAACGAAAGAGCTAAACTTCTCACATTCCATTTCTGAAAACTTTTCCAAA
CAATGTGAAAGCACAGTAAGGAAAAGTGAACTGAGTGGCTGGGACTATGAATATGGTTTC
TGCTTACCCAAGACACCCCGATGTGCTCCTGAACCAGATGCTTTTAATCCCTGTGAAGAC
ATTATGGGCTATGACTTCCTTAGGGTCCTGATTTGGCTGATTAATATTCTAGCCATCATG
GGAAACATGACTGTTCTTTTTGTTCTCCTGACAAGTCGTTACAAACTTACAGTGCCTCGT
TTTCTCATGTGCAATCTCTCCTTTGCAGACTTTTGCATGGGGCTCTATCTGCTGCTCATA
GCCTCAGTTGATTCCCAAACCAAGGGCCAGTACTATAACCATGCCATAGACTGGCAGACA
GGGAGTGGGTGCAGCACTGCTGGCTTTTTCACTGTATTAGCAAGTGAACTTTCTGTCTAC
ACCCTCACCGTCATCACTCTAGAAAGATGGCACACCATCACCTATGCTATTCACCTGGAC
CAAAAGCTGCGATTAAGACATGCCATTCTGATTATGCTTGGAGGCTGGCTCTTTTCTTCT
CTAATTGCTATGTTGCCCCTTGTCGGGGTCAGCAATTACATGAAGGTCAGTATTTGCTTC
CCCATGGATGTGGAAACCACTCTCTCACAAGTCTATATATTAACCATCCTGATTCTCAAT
GTGGTGGCCTTCTTAATAATTTGTGCTTGCTACATTAAAATTTATTTTGCAGTTCGAAAC
CCAGAATTAATGGCTACCAATAAAGATACAAAGATTGCTAAGAAAATGGCAATCCTCATC
TTCACCGATTTTACCTGCATGGCACCTATCTCTTTTTTTGCCATCTCAGCTGCCTTCAAA
GTACCTCTTATCACAGTAACCAACTCTAAAGTTTTACTGGTTCTTTTTTATCCCATCAAT
TCTTGTGCCAATCCATTTCTGTATGCAATATTCACTAAGACATTCCAAAGAGATTTCTTT
CTTTTGCTGAGCAAATTTGGCTGCTGTAAACGTCGGGCTGATCCTCTTTATAGAAGGAAA
GATTTTTCAGCTTACACCTCCAACTGCAAAAATGGCTTCACTGGATCAAATAAGCCTTCT
CAATCCACCTTGAAGTTGTCCACATTGCACTGTCAAGGTACAGCTCTCCTAGACAAGACT
CGCTACACAGAGTGTTAA
Target 1 GenBank Gene ID
Target 1 GeneCard ID LHCGR Link Image
Target 1 GenAtlas ID LHCGR Link Image
Target 1 HGNC ID HGNC:6585 Link Image
Target 1 Chromosome Location 2
Target 1 Locus 2p21
Target 1 SNPs SNPJam Report Link Image
Target 1 General References
  1. Liu G, Duranteau L, Carel JC, Monroe J, Doyle DA, Shenker A: Leydig-cell tumors caused by an activating mutation of the gene encoding the luteinizing hormone receptor. N Engl J Med. 1999 Dec 2;341(23):1731-6. [PubMed Link Image]
  2. Jia XC, Oikawa M, Bo M, Tanaka T, Ny T, Boime I, Hsueh AJ: Expression of human luteinizing hormone (LH) receptor: interaction with LH and chorionic gonadotropin from human but not equine, rat, and ovine species. Mol Endocrinol. 1991 Jun;5(6):759-68. [PubMed Link Image]
  3. Minegishi T, Nakamura K, Takakura Y, Miyamoto K, Hasegawa Y, Ibuki Y, Igarashi M, Minegish T [corrected to Minegishi T: Cloning and sequencing of human LH/hCG receptor cDNA. Biochem Biophys Res Commun. 1990 Nov 15;172(3):1049-54. [PubMed Link Image]
  4. Frazier AL, Robbins LS, Stork PJ, Sprengel R, Segaloff DL, Cone RD: Isolation of TSH and LH/CG receptor cDNAs from human thyroid: regulation by tissue specific splicing. Mol Endocrinol. 1990 Aug;4(8):1264-76. [PubMed Link Image]
  5. Atger M, Misrahi M, Sar S, Le Flem L, Dessen P, Milgrom E: Structure of the human luteinizing hormone-choriogonadotropin receptor gene: unusual promoter and 5' non-coding regions. Mol Cell Endocrinol. 1995 Jun;111(2):113-23. [PubMed Link Image]
  6. Latronico AC, Anasti J, Arnhold IJ, Mendonca BB, Domenice S, Albano MC, Zachman K, Wajchenberg BL, Tsigos C: A novel mutation of the luteinizing hormone receptor gene causing male gonadotropin-independent precocious puberty. J Clin Endocrinol Metab. 1995 Aug;80(8):2490-4. [PubMed Link Image]
  7. Shenker A, Laue L, Kosugi S, Merendino JJ Jr, Minegishi T, Cutler GB Jr: A constitutively activating mutation of the luteinizing hormone receptor in familial male precocious puberty. Nature. 1993 Oct 14;365(6447):652-4. [PubMed Link Image]
  8. Yano K, Saji M, Hidaka A, Moriya N, Okuno A, Kohn LD, Cutler GB Jr: A new constitutively activating point mutation in the luteinizing hormone/choriogonadotropin receptor gene in cases of male-limited precocious puberty. J Clin Endocrinol Metab. 1995 Apr;80(4):1162-8. [PubMed Link Image]
  9. Kremer H, Kraaij R, Toledo SP, Post M, Fridman JB, Hayashida CY, van Reen M, Milgrom E, Ropers HH, Mariman E, et al.: Male pseudohermaphroditism due to a homozygous missense mutation of the luteinizing hormone receptor gene. Nat Genet. 1995 Feb;9(2):160-4. [PubMed Link Image]
  10. Kosugi S, Van Dop C, Geffner ME, Rabl W, Carel JC, Chaussain JL, Mori T, Merendino JJ Jr, Shenker A: Characterization of heterogeneous mutations causing constitutive activation of the luteinizing hormone receptor in familial male precocious puberty. Hum Mol Genet. 1995 Feb;4(2):183-8. [PubMed Link Image]
  11. 8281137 Kremer H, Mariman E, Otten BJ, Moll GW Jr, Stoelinga GB, Wit JM, Jansen M, Drop SL, Faas B, Ropers HH, et al.: Cosegregation of missense mutations of the luteinizing hormone receptor gene with familial male-limited precocious puberty. Hum Mol Genet. 1993 Nov;2(11):1779-83.
  12. 8559204 Latronico AC, Anasti J, Arnhold IJ, Rapaport R, Mendonca BB, Bloise W, Castro M, Tsigos C, Chrousos GP: Brief report: testicular and ovarian resistance to luteinizing hormone caused by inactivating mutations of the luteinizing hormone-receptor gene. N Engl J Med. 1996 Feb 22;334(8):507-12.
  13. 8747461 Jiang X, Dreano M, Buckler DR, Cheng S, Ythier A, Wu H, Hendrickson WA, el Tayar N: Structural predictions for the ligand-binding region of glycoprotein hormone receptors and the nature of hormone-receptor interactions. Structure. 1995 Dec 15;3(12):1341-53.
  14. 8829636 Cocco S, Meloni A, Marini MG, Cao A, Moi P: A missense (T577I) mutation in the luteinizing hormone receptor gene associated with familial male-limited precocious puberty. Hum Mutat. 1996;7(2):164-6.
  15. 8929952 Evans BA, Bowen DJ, Smith PJ, Clayton PE, Gregory JW: A new point mutation in the luteinising hormone receptor gene in familial and sporadic male limited precocious puberty: genotype does not always correlate with phenotype. J Med Genet. 1996 Feb;33(2):143-7.
  16. 9215288 Misrahi M, Meduri G, Pissard S, Bouvattier C, Beau I, Loosfelt H, Jolivet A, Rappaport R, Milgrom E, Bougneres P: Comparison of immunocytochemical and molecular features with the phenotype in a case of incomplete male pseudohermaphroditism associated with a mutation of the luteinizing hormone receptor. J Clin Endocrinol Metab. 1997 Jul;82(7):2159-65.
  17. 9467560 Gromoll J, Partsch CJ, Simoni M, Nordhoff V, Sippell WG, Nieschlag E, Saxena BB: A mutation in the first transmembrane domain of the lutropin receptor causes male precocious puberty. J Clin Endocrinol Metab. 1998 Feb;83(2):476-80.
  18. 9514160 Latronico AC, Chai Y, Arnhold IJ, Liu X, Mendonca BB, Segaloff DL: A homozygous microdeletion in helix 7 of the luteinizing hormone receptor associated with familial testicular and ovarian resistance is due to both decreased cell surface expression and impaired effector activation by the cell surface receptor. Mol Endocrinol. 1998 Mar;12(3):442-50.
  19. 9626144 Stavrou SS, Zhu YS, Cai LQ, Katz MD, Herrera C, Defillo-Ricart M, Imperato-McGinley J: A novel mutation of the human luteinizing hormone receptor in 46XY and 46XX sisters. J Clin Endocrinol Metab. 1998 Jun;83(6):2091-8.
  20. 9626653 Martens JW, Verhoef-Post M, Abelin N, Ezabella M, Toledo SP, Brunner HG, Themmen AP: A homozygous mutation in the luteinizing hormone receptor causes partial Leydig cell hypoplasia: correlation between receptor activity and phenotype. Mol Endocrinol. 1998 Jun;12(6):775-84.
  21. 9661624 Latronico AC, Abell AN, Arnhold IJ, Liu X, Lins TS, Brito VN, Billerbeck AE, Segaloff DL, Mendonca BB: A unique constitutively activating mutation in third transmembrane helix of luteinizing hormone receptor causes sporadic male gonadotropin-independent precocious puberty. J Clin Endocrinol Metab. 1998 Jul;83(7):2435-40.
  22. 9851790 Rodien P, Cetani F, Costagliola S, Tonacchera M, Duprez L, Minegishi T, Govaerts C, Vassart G: Evidences for an allelic variant of the human LC/CG receptor rather than a gene duplication: functional comparison of wild-type and variant receptors. J Clin Endocrinol Metab. 1998 Dec;83(12):4431-4.
  23. 9858858 Tsai-Morris CH, Geng Y, Buczko E, Dehejia A, Dufau ML: Genomic distribution and gonadal mRNA expression of two human luteinizing hormone receptor exon 1 sequences in random populations. Hum Hered. 1999 Jan;49(1):48-51.
Target 1 Drug References
  1. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed Link Image]
  2. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed Link Image]
Drug Target 2 [top]
Target 2 ID 226
Target 2 Name Gonadotropin-releasing hormone receptor
Target 2 Synonyms
  1. GnRH receptor
  2. GnRH-R
Target 2 Gene Name GNRHR
Target 2 Protein Sequence >Gonadotropin-releasing hormone receptor 
MANSASPEQNQNHCSAINNSIPLMQGNLPTLTLSGKIRVTVTFFLFLLSATFNASFLLKL
QKWTQKKEKGKKLSRMKLLLKHLTLANLLETLIVMPLDGMWNITVQWYAGELLCKVLSYL
KLFSMYAPAFMMVVISLDRSLAITRPLALKSNSKVGQSMVGLAWILSSVFAGPQLYIFRM
IHLADSSGQTKVFSQCVTHCSFSQWWHQAFYNFFTFSCLFIIPLFIMLICNAKIIFTLTR
VLHQDPHELQLNQSKNNIPRARLKTLKMTVAFATSFTVCWTPYYVLGIWYWFDPEMLNRL
SDPVNHFFFLFAFLNPCFDPLIYGYFSL
Target 2 Number of Residues 333
Target 2 Molecular Weight 37731
Target 2 Theoretical pI 9.93
Target 2 GO Classification
Function
protein-hormone receptor activity
gonadotropin-releasing hormone receptor activity
signal transducer activity
receptor activity
transmembrane receptor activity
G-protein coupled receptor activity
rhodopsin-like receptor activity
Process
cellular process
cell communication
signal transduction
cell surface receptor linked signal transduction
G-protein coupled receptor protein signaling pathway
Component
cell
membrane
intrinsic to membrane
integral to membrane
Target 2 General Function Involved in rhodopsin-like receptor activity
Target 2 Specific Function Receptor 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-calcium second messenger system. Isoform 2 may act a an inhibitor of GnRH-R signaling
Target 2 Pathways Not Available
Target 2 Reactions Not Available
Target 2 Pfam Domain Function
Target 2 Signals
  • None
Target 2 Transmembrane Regions
  • 39-58
  • 78-97
  • 116-137
  • 165-184
  • 213-232
  • 282-300
  • 307-326
Target 2 Essentiality Non-Essential
Target 2 GenBank ID Protein 183422 Link Image
Target 2 UniProtKB/Swiss-Prot ID P30968 Link Image
Target 2 UniProtKB/Swiss-Prot Entry Name GNRHR_HUMAN Link Image
Target 2 PDB ID Not Available
Target 2 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 2 Gene Sequence >987 bp 
ATGGCAAACAGTGCCTCTCCTGAACAGAATCAAAATCACTGTTCAGCCATCAACAACAGC
ATCCCACTGATGCAGGGCAACCTCCCCACTCTGACCTTGTCTGGAAAGATCCGAGTGACG
GTTACTTTCTTCCTTTTTCTGCTCTCTGCGACCTTTAATGCTTCTTTCTTGTTGAAACTT
CAGAAGTGGACACAGAAGAAAGAGAAAGGGAAAAAGCTCTCAAGAATGAAGCTGCTCTTA
AAACATCTGACCTTAGCCAACCTGTTGGAGACTCTGATTGTCATGCCACTGGATGGGATG
TGGAACATTACAGTCCAATGGTATGCTGGAGAGTTACTCTGCAAAGTTCTCAGTTATCTA
AAGCTTTTCTCCATGTATGCCCCAGCCTTCATGATGGTGGTGATCAGCCTGGACCGCTCC
CTGGCTATCACGAGGCCCCTAGCTTTGAAAAGCAACAGCAAAGTCGGACAGTCCATGGTT
GGCCTGGCCTGGATCCTCAGTAGTGTCTTTGCAGGACCACAGTTATACATCTTCAGGATG
ATTCATCTAGCAGACAGCTCTGGACAGACAAAAGTTTTCTCTCAATGTGTAACACACTGC
AGTTTTTCACAATGGTGGCATCAAGCATTTTATAACTTTTTCACCTTCAGCTGCCTCTTC
ATCATCCCTCTTTTCATCATGCTGATCTGCAATGCAAAAATCATCTTCACCCTGACACGG
GTCCTTCATCAGGACCCCCACGAACTACAACTGAATCAGTCCAAGAACAATATACCAAGA
GCACGGCTGAAGACTCTAAAAATGACGGTTGCATTTGCCACTTCATTTACTGTCTGCTGG
ACTCCCTACTATGTCCTAGGAATTTGGTATTGGTTTGATCCTGAAATGTTAAACAGGTTG
TCAGACCCAGTAAATCACTTCTTCTTTCTCTTTGCCTTTTTAAACCCATGCTTTGATCCA
CTTATCTATGGATATTTTTCTCTGTGA
Target 2 GenBank Gene ID
Target 2 GeneCard ID GNRHR Link Image
Target 2 GenAtlas ID GNRHR Link Image
Target 2 HGNC ID HGNC:4421 Link Image
Target 2 Chromosome Location 4
Target 2 Locus 4q21.2
Target 2 SNPs SNPJam Report Link Image
Target 2 General References
  1. Kottler ML, Bergametti F, Carre MC, Morice S, Decoret E, Lagarde JP, Starzec A, Counis R: Tissue-specific pattern of variant transcripts of the human gonadotropin-releasing hormone receptor gene. Eur J Endocrinol. 1999 Jun;140(6):561-9. [PubMed Link Image]
  2. Kakar SS, Musgrove LC, Devor DC, Sellers JC, Neill JD: Cloning, sequencing, and expression of human gonadotropin releasing hormone (GnRH) receptor. Biochem Biophys Res Commun. 1992 Nov 30;189(1):289-95. [PubMed Link Image]
  3. Kakar SS, Grizzle WE, Neill JD: The nucleotide sequences of human GnRH receptors in breast and ovarian tumors are identical with that found in pituitary. Mol Cell Endocrinol. 1994 Dec;106(1-2):145-9. [PubMed Link Image]
  4. Chi L, Zhou W, Prikhozhan A, Flanagan C, Davidson JS, Golembo M, Illing N, Millar RP, Sealfon SC: Cloning and characterization of the human GnRH receptor. Mol Cell Endocrinol. 1993 Feb;91(1-2):R1-6. [PubMed Link Image]
  5. Grosse R, Schoneberg T, Schultz G, Gudermann T: Inhibition of gonadotropin-releasing hormone receptor signaling by expression of a splice variant of the human receptor. Mol Endocrinol. 1997 Aug;11(9):1305-18. [PubMed Link Image]
  6. Kakar SS: Molecular structure of the human gonadotropin-releasing hormone receptor gene. Eur J Endocrinol. 1997 Aug;137(2):183-92. [PubMed Link Image]
Target 2 Drug References
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  2. Volker P, Grundker C, Schmidt O, Schulz KD, Emons G: Expression of receptors for luteinizing hormone-releasing hormone in human ovarian and endometrial cancers: frequency, autoregulation, and correlation with direct antiproliferative activity of luteinizing hormone-releasing hormone analogues. Am J Obstet Gynecol. 2002 Feb;186(2):171-9. [PubMed Link Image]
  3. Zapatero-Caballero H, Sanchez-Franco F, Guerra-Perez N, Fernandez-Mendez C, Fernandez-Vazquez G: Gonadotropin-releasing hormone receptor gene expression during pubertal development of male rats. Biol Reprod. 2003 May;68(5):1764-70. Epub 2002 Dec 11. [PubMed Link Image]
  4. Zapatero-Caballero H, Sanchez-Franco F, Fernandez-Mendez C, Garcia-San Frutos M, Botella-Cubells LM, Fernandez-Vazquez G: Gonadotropin-releasing hormone receptor gene expression during pubertal development of female rats. Biol Reprod. 2004 Feb;70(2):348-55. Epub 2003 Oct 15. [PubMed Link Image]
  5. Roth C, Hegemann F, Hildebrandt J, Balzer I, Witt A, Wuttke W, Jarry H: Pituitary and gonadal effects of GnRH (gonadotropin releasing hormone) analogues in two peripubertal female rat models. Pediatr Res. 2004 Jan;55(1):126-33. Epub 2003 Nov 6. [PubMed Link Image]
  6. Castellon E, Clementi M, Hitschfeld C, Sanchez C, Benitez D, Saenz L, Contreras H, Huidobro C: Effect of leuprolide and cetrorelix on cell growth, apoptosis, and GnRH receptor expression in primary cell cultures from human prostate carcinoma. Cancer Invest. 2006 Apr-May;24(3):261-8. [PubMed Link Image]

This project is supported by Genome Alberta & Genome Canada, a not-for-profit organization that is leading Canada's national genomics strategy with $600 million in funding from the federal government. This project is also supported in part by GenomeQuest, Inc., an enterprise genomic information company serving the life science community.