14
| AHFS_Codes | - |
| ATC_Codes | L02AE03 |
| Absorption | Inactive orally, rapidly absorbed following subcutaneous administration |
| Biotransformation | Hepatic |
| Brand_Mixtures | Not Available |
| Brand_Names | Zoladex |
| CAS_Registry_Number | 65807-02-5 |
| ChEBI_ID | Not Available |
| Chemical_Formula | C59H84N18O14 |
| Chemical_IUPAC_Name | Not Available |
| Chemical_Structure | Not Available |
| Creation_Date | 2005-06-13 07:24:05 -0600 |
| DPD_Drug_ID_Number | 2225905 |
| Description | Goserelin is a synthetic hormone. In men, it stops the production of the hormone testosterone, which may stimulate the growth of cancer cells. In women, goserelin decreases the production of the hormone estradiol (which may stimulate the growth of cancer cells) to levels similar to a postmenopausal state. When the medication is stopped, hormone levels return to normal. |
| Dosage_Forms | Implant Subcutaneous |
| Drug_Category | Antineoplastic Agents<br />Antineoplastic Agents, Hormonal |
| Drug_Interactions | Not Available |
| Drug_Reference | Not Available |
| Drug_Type | Approved<br />Biotech |
| Experimental_Caco2_Permeability | Not Available |
| Experimental_LogP_Hydrophobicity | -2 |
| Experimental_Logs | Not Available |
| Experimental_Water_Solubility | Soluble |
| Food_Interactions | Not Available |
| GenBank_ID | Not Available |
| Generic_Name | Goserelin |
| HET_ID | Not Available |
| Half_Life | 4-5 hours |
| InChI_Identifier | Not Available |
| InChI_Key | Not Available |
| Indication | Breast cancer; Prostate carcinoma; Endometriosis |
| KEGG_Compound_ID | Not Available |
| KEGG_Drug_ID | D00573 |
| LIMS_Drug_ID | 14 |
| Mechanism_Of_Action | ZOLADEX is a synthetic decapeptide analogue of LHRH. ZOLADEX acts as a potent inhibitor of pituitary gonadotropin secretion when administered in the biodegradable formulation. The result is sustained suppression of LH and serum testosterone levels. |
| Melting_Point | Not Available |
| Molecular_Weight_Avg | 1269.4105 |
| Molecular_Weight_Mono | Not Available |
| Organisms_Affected | Humans and other mammals |
| PDB_Experimental_ID | Not Available |
| PDB_Homology_ID | Not Available |
| PDRhealth_Link | Not Available |
| Pathways | Not Available |
| PharmGKB_ID | Not Available |
| Pharmacology | The pharmacokinetics of ZOLADEX have been determined in both male and female healthy volunteers and patients. In these studies, ZOLADEX was administered as a single 250&micro;g (aqueous solution) dose and as a single or multiple 3.6 mg depot dose by subcutaneous route. |
| Predicted_LogP_Hydrophobicity | Not Available |
| Predicted_LogS | Not Available |
| Predicted_Water_Solubility | Not Available |
| Primary_Accession_No | DB00014 |
| Protein_Binding | 27.3% |
| PubChem_Compound_ID | Not Available |
| PubChem_Substance_ID | Not Available |
| RxList_Link | <a href="http://www.rxlist.com/cgi/generic/goserel.htm" target="_blank">http://www.rxlist.com/cgi/generic/goserel.htm</a> |
| Secondary_Accession_No | BIOD00113<br />BTD00113 |
| Smiles_String_canonical | Not Available |
| Smiles_String_isomeric | Not Available |
| State | solid |
| Structure | false |
| SwissProt_ID | Not Available |
| SwissProt_Name | Not Available |
| Synonyms | Goserelin acetate<br />Goserelin acetate (JAN/USP) |
| Synthesis_Reference | Not Available |
| Toxicity | No experience of overdosage from clinical trials |
| Update_Date | 2010-09-29 14:34:47 -0600 |
| Wikipedia_Link | <a href="http://en.wikipedia.org/wiki/Goserelin" target="_blank">http://en.wikipedia.org/wiki/Goserelin</a> |
| pKa_Isoelectric_Point | Not Available |
| Drug_Target_1_Cellular_Location | Membrane<br />multi-pass membrane protein |
| Drug_Target_1_Chromosome_Location | Not Available |
| Drug_Target_1_Drug_References | 17016423 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.<br />17139284 Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.<br />20053189 Kirby RS, Fitzpatrick JM, Clarke N: Abarelix and other gonadotrophin-releasing hormone antagonists in prostate cancer. BJU Int. 2009 Dec;104(11):1580-4. |
| Drug_Target_1_Essentiality | Non-Essential |
| Drug_Target_1_GenAtlas_ID | LHCGR |
| Drug_Target_1_GenBank_ID_Gene | M73746 |
| Drug_Target_1_GenBank_ID_Protein | 903746 |
| Drug_Target_1_GeneCard_ID | LHCGR |
| Drug_Target_1_Gene_Name | LHCGR |
| Drug_Target_1_Gene_Sequence | >2058 bp<br />ATGAAGCAGCGGTTCTCGCCGCTGCAGCTGCTGAAGCTGCTGCTGCTGCTGCAGGCGCCG<br />CTGCCACGAGCGCTGCGCAGGCTCTGCCCTGAGCCCTGCAACTGCGTGCCCGACGGCGCC<br />CTGCGTGCCCCGGCCCCACGGCCGTCCACTCGACTATCACTTGCCTACCTCCCTGTCAAA<br />GTGATCCCATCTCAAAGTTTCAGAGGACTTAATGAGGTCATAAAAATTGAAATCTCTCAG<br />ATTGATTCCCTGGAAAGGATAGAAGCTAATGCCTTTGACAACCTCCTCAATTTGTCTGAA<br />ATACTGATCCAGAACACCAAAAATCTGAGATACATTGAGCCCGGAGCATTTATAAATCTT<br />CCCCGATTAAAATACTTGAGCATCTGTAACACAGGCATCAGAAAGTTTCCAGATGTTACG<br />AAGGTCTTCTCCTCTGAATCAAATTTCATTCTGGAAATTTGTGATAACTTACACATAACC<br />ACCATACCAGGAAATGCTTTTCAAGGGATGAATAATGAATCTGTAACACTCAAACTATAT<br />GGAAATGGATTTGAAGAAGTACAAAGTCATGCATTCAATGGGACGACACTGACTTCACTG<br />GAGCTAAAGGAAAACGTACATCTGGAGAAGATGCACAATGGAGCCTTCCGTGGGGCCACA<br />GGGCCGAAAACCTTGGATATTTCTTCCACCAAATTGCAGGCCCTGCCGAGCTATGGCCTA<br />GAGTCCATTCAGAGGCTAATTGCCACGTCATCCTATTCTCTAAAAAAATTGCCATCAAAA<br />CAAACATTTGTCAATCTCCTGAGGGCCACGCTTCATTACCCCAGCCACTGCTGTGCATTT<br />AGAAACTTGCCAACGAAAGAGCTAAACTTCTCACATTCCATTTCTGAAAACTTTTCCAAA<br />CAATGTGAAAGCACAGTAAGGAAAAGTGAACTGAGTGGCTGGGACTATGAATATGGTTTC<br />TGCTTACCCAAGACACCCCGATGTGCTCCTGAACCAGATGCTTTTAATCCCTGTGAAGAC<br />ATTATGGGCTATGACTTCCTTAGGGTCCTGATTTGGCTGATTAATATTCTAGCCATCATG<br />GGAAACATGACTGTTCTTTTTGTTCTCCTGACAAGTCGTTACAAACTTACAGTGCCTCGT<br />TTTCTCATGTGCAATCTCTCCTTTGCAGACTTTTGCATGGGGCTCTATCTGCTGCTCATA<br />GCCTCAGTTGATTCCCAAACCAAGGGCCAGTACTATAACCATGCCATAGACTGGCAGACA<br />GGGAGTGGGTGCAGCACTGCTGGCTTTTTCACTGTATTAGCAAGTGAACTTTCTGTCTAC<br />ACCCTCACCGTCATCACTCTAGAAAGATGGCACACCATCACCTATGCTATTCACCTGGAC<br />CAAAAGCTGCGATTAAGACATGCCATTCTGATTATGCTTGGAGGCTGGCTCTTTTCTTCT<br />CTAATTGCTATGTTGCCCCTTGTCGGGGTCAGCAATTACATGAAGGTCAGTATTTGCTTC<br />CCCATGGATGTGGAAACCACTCTCTCACAAGTCTATATATTAACCATCCTGATTCTCAAT<br />GTGGTGGCCTTCTTAATAATTTGTGCTTGCTACATTAAAATTTATTTTGCAGTTCGAAAC<br />CCAGAATTAATGGCTACCAATAAAGATACAAAGATTGCTAAGAAAATGGCAATCCTCATC<br />TTCACCGATTTTACCTGCATGGCACCTATCTCTTTTTTTGCCATCTCAGCTGCCTTCAAA<br />GTACCTCTTATCACAGTAACCAACTCTAAAGTTTTACTGGTTCTTTTTTATCCCATCAAT<br />TCTTGTGCCAATCCATTTCTGTATGCAATATTCACTAAGACATTCCAAAGAGATTTCTTT<br />CTTTTGCTGAGCAAATTTGGCTGCTGTAAACGTCGGGCTGATCCTCTTTATAGAAGGAAA<br />GATTTTTCAGCTTACACCTCCAACTGCAAAAATGGCTTCACTGGATCAAATAAGCCTTCT<br />CAATCCACCTTGAAGTTGTCCACATTGCACTGTCAAGGTACAGCTCTCCTAGACAAGACT<br />CGCTACACAGAGTGTTAA |
| Drug_Target_1_General_Function | Involved in rhodopsin-like receptor activity |
| Drug_Target_1_General_References | 10580072 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.<br />1922095 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.<br />2244890 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.<br />2293030 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.<br />7556872 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.<br />7629248 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.<br />7692306 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.<br />7714085 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.<br />7719343 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.<br />7757065 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.<br />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.<br />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.<br />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.<br />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.<br />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.<br />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.<br />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.<br />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.<br />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.<br />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.<br />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.<br />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.<br />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. |
| Drug_Target_1_HGNC_ID | HGNC:6585 |
| Drug_Target_1_HPRD_ID | 01073 |
| Drug_Target_1_ID | 148 |
| Drug_Target_1_Locus | 2p21 |
| Drug_Target_1_Molecular_Weight | 78617 |
| Drug_Target_1_Name | Lutropin-choriogonadotropic hormone receptor |
| Drug_Target_1_Number_of_Residues | 710 |
| Drug_Target_1_PDB_ID | Not Available |
| Drug_Target_1_Pathway | Not Available |
| Drug_Target_1_Pfam_Domain_Function | PF00001 7tm_1 |
| Drug_Target_1_Protein_Sequence | >Lutropin-choriogonadotropic hormone receptor precursor<br />MKQRFSALQLLKLLLLLQPPLPRALREALCPEPCNCVPDGALRCPGPTAGLTRLSLAYLP<br />VKVIPSQAFRGLNEVIKIEISQIDSLERIEANAFDNLLNLSEILIQNTKNLRYIEPGAFI<br />NLPRLKYLSICNTGIRKFPDVTKVFSSESNFILEICDNLHITTIPGNAFQGMNNESVTLK<br />LYGNGFEEVQSHAFNGTTLTSLELKENVHLEKMHNGAFRGATGPKTLDISSTKLQALPSY<br />GLESIQRLIATSSYSLKKLPSRETFVNLLEATLTYPSHCCAFRNLPTKEQNFSHSISENF<br />SKQCESTVRKVSNKTLYSSMLAESELSGWDYEYGFCLPKTPRCAPEPDAFNPCEDIMGYD<br />FLRVLIWLINILAIMGNMTVLFVLLTSRYKLTVPRFLMCNLSFADFCMGLYLLLIASVDS<br />QTKGQYYNHAIDWQTGSGCSTAGFFTVFASELSVYTLTVITLERWHTITYAIHLDQKLRL<br />RHAILIMLGGWLFSSLIAMLPLVGVSNYMKVSICFPMDVETTLSQVYILTILILNVVAFF<br />IICACYIKIYFAVRNPELMATNKDTKIAKKMAILIFTDFTCMAPISFFAISAAFKVPLIT<br />VTNSKVLLVLFYPINSCANPFLYAIFTKTFQRDFFLLLSKFGCCKRRAELYRRKDFSAYT<br />SNCKNGFTGSNKPSQSTLKLSTLHCQGTALLDKTRYTEC |
| Drug_Target_1_Reaction | Not Available |
| Drug_Target_1_Signals | 1-26 |
| Drug_Target_1_Specific_Function | Receptor for lutropin-choriogonadotropic hormone. The activity of this receptor is mediated by G proteins which activate adenylate cyclase |
| Drug_Target_1_SwissProt_ID | P22888 |
| Drug_Target_1_SwissProt_Name | LSHR_HUMAN |
| Drug_Target_1_Synonyms | LH/CG-R<br />LHR<br />LSH- R<br />Luteinizing hormone receptor<br />Lutropin-choriogonadotropic hormone receptor precursor |
| Drug_Target_1_Theoretical_pI | 8.58 |
| Drug_Target_1_Transmembrane_Regions | 364-385<br />396-416<br />440-462<br />483-505<br />526-549<br />571-594<br />606-627 |
| Drug_Target_2_Cellular_Location | Membrane<br />multi-pass membrane protein |
| Drug_Target_2_Chromosome_Location | Not Available |
| Drug_Target_2_Drug_References | 20053189 Kirby RS, Fitzpatrick JM, Clarke N: Abarelix and other gonadotrophin-releasing hormone antagonists in prostate cancer. BJU Int. 2009 Dec;104(11):1580-4. |
| Drug_Target_2_Essentiality | Non-Essential |
| Drug_Target_2_GenAtlas_ID | GNRHR |
| Drug_Target_2_GenBank_ID_Gene | L03380 |
| Drug_Target_2_GenBank_ID_Protein | 183422 |
| Drug_Target_2_GeneCard_ID | GNRHR |
| Drug_Target_2_Gene_Name | GNRHR |
| Drug_Target_2_Gene_Sequence | >987 bp<br />ATGGCAAACAGTGCCTCTCCTGAACAGAATCAAAATCACTGTTCAGCCATCAACAACAGC<br />ATCCCACTGATGCAGGGCAACCTCCCCACTCTGACCTTGTCTGGAAAGATCCGAGTGACG<br />GTTACTTTCTTCCTTTTTCTGCTCTCTGCGACCTTTAATGCTTCTTTCTTGTTGAAACTT<br />CAGAAGTGGACACAGAAGAAAGAGAAAGGGAAAAAGCTCTCAAGAATGAAGCTGCTCTTA<br />AAACATCTGACCTTAGCCAACCTGTTGGAGACTCTGATTGTCATGCCACTGGATGGGATG<br />TGGAACATTACAGTCCAATGGTATGCTGGAGAGTTACTCTGCAAAGTTCTCAGTTATCTA<br />AAGCTTTTCTCCATGTATGCCCCAGCCTTCATGATGGTGGTGATCAGCCTGGACCGCTCC<br />CTGGCTATCACGAGGCCCCTAGCTTTGAAAAGCAACAGCAAAGTCGGACAGTCCATGGTT<br />GGCCTGGCCTGGATCCTCAGTAGTGTCTTTGCAGGACCACAGTTATACATCTTCAGGATG<br />ATTCATCTAGCAGACAGCTCTGGACAGACAAAAGTTTTCTCTCAATGTGTAACACACTGC<br />AGTTTTTCACAATGGTGGCATCAAGCATTTTATAACTTTTTCACCTTCAGCTGCCTCTTC<br />ATCATCCCTCTTTTCATCATGCTGATCTGCAATGCAAAAATCATCTTCACCCTGACACGG<br />GTCCTTCATCAGGACCCCCACGAACTACAACTGAATCAGTCCAAGAACAATATACCAAGA<br />GCACGGCTGAAGACTCTAAAAATGACGGTTGCATTTGCCACTTCATTTACTGTCTGCTGG<br />ACTCCCTACTATGTCCTAGGAATTTGGTATTGGTTTGATCCTGAAATGTTAAACAGGTTG<br />TCAGACCCAGTAAATCACTTCTTCTTTCTCTTTGCCTTTTTAAACCCATGCTTTGATCCA<br />CTTATCTATGGATATTTTTCTCTGTGA |
| Drug_Target_2_General_Function | Involved in rhodopsin-like receptor activity |
| Drug_Target_2_General_References | 10366411 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.<br />1333190 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.<br />7534732 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.<br />8386108 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.<br />9259321 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.<br />9272108 Kakar SS: Molecular structure of the human gonadotropin-releasing hormone receptor gene. Eur J Endocrinol. 1997 Aug;137(2):183-92. |
| Drug_Target_2_HGNC_ID | HGNC:4421 |
| Drug_Target_2_HPRD_ID | 00732 |
| Drug_Target_2_ID | 226 |
| Drug_Target_2_Locus | 4q21.2 |
| Drug_Target_2_Molecular_Weight | 37731 |
| Drug_Target_2_Name | Gonadotropin-releasing hormone receptor |
| Drug_Target_2_Number_of_Residues | 333 |
| Drug_Target_2_PDB_ID | Not Available |
| Drug_Target_2_Pathway | Not Available |
| Drug_Target_2_Pfam_Domain_Function | PF00001 7tm_1 |
| Drug_Target_2_Protein_Sequence | >Gonadotropin-releasing hormone receptor<br />MANSASPEQNQNHCSAINNSIPLMQGNLPTLTLSGKIRVTVTFFLFLLSATFNASFLLKL<br />QKWTQKKEKGKKLSRMKLLLKHLTLANLLETLIVMPLDGMWNITVQWYAGELLCKVLSYL<br />KLFSMYAPAFMMVVISLDRSLAITRPLALKSNSKVGQSMVGLAWILSSVFAGPQLYIFRM<br />IHLADSSGQTKVFSQCVTHCSFSQWWHQAFYNFFTFSCLFIIPLFIMLICNAKIIFTLTR<br />VLHQDPHELQLNQSKNNIPRARLKTLKMTVAFATSFTVCWTPYYVLGIWYWFDPEMLNRL<br />SDPVNHFFFLFAFLNPCFDPLIYGYFSL |
| Drug_Target_2_Reaction | Not Available |
| Drug_Target_2_Signals | None |
| Drug_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 |
| Drug_Target_2_SwissProt_ID | P30968 |
| Drug_Target_2_SwissProt_Name | GNRHR_HUMAN |
| Drug_Target_2_Synonyms | GnRH receptor<br />GnRH-R |
| Drug_Target_2_Theoretical_pI | 9.93 |
| Drug_Target_2_Transmembrane_Regions | 39-58<br />78-97<br />116-137<br />165-184<br />213-232<br />282-300<br />307-326 |
| Drug_Target_3_Cellular_Location | - |
| Drug_Target_3_Chromosome_Location | - |
| Drug_Target_3_Drug_References | - |
| Drug_Target_3_Essentiality | - |
| Drug_Target_3_GenAtlas_ID | - |
| Drug_Target_3_GenBank_ID_Gene | - |
| Drug_Target_3_GenBank_ID_Protein | - |
| Drug_Target_3_GeneCard_ID | - |
| Drug_Target_3_Gene_Name | - |
| Drug_Target_3_Gene_Sequence | - |
| Drug_Target_3_General_Function | - |
| Drug_Target_3_General_References | - |
| Drug_Target_3_HGNC_ID | - |
| Drug_Target_3_HPRD_ID | - |
| Drug_Target_3_ID | - |
| Drug_Target_3_Locus | - |
| Drug_Target_3_Molecular_Weight | - |
| Drug_Target_3_Name | - |
| Drug_Target_3_Number_of_Residues | - |
| Drug_Target_3_PDB_ID | - |
| Drug_Target_3_Pathway | - |
| Drug_Target_3_Pfam_Domain_Function | - |
| Drug_Target_3_Protein_Sequence | - |
| Drug_Target_3_Reaction | - |
| Drug_Target_3_Signals | - |
| Drug_Target_3_Specific_Function | - |
| Drug_Target_3_SwissProt_ID | - |
| Drug_Target_3_SwissProt_Name | - |
| Drug_Target_3_Synonyms | - |
| Drug_Target_3_Theoretical_pI | - |
| Drug_Target_3_Transmembrane_Regions | - |
| Phase_1_Metabolizing_Enzyme_1_Gene_Name | - |
| Phase_1_Metabolizing_Enzyme_1_ID | - |
| Phase_1_Metabolizing_Enzyme_1_Name | - |
| Phase_1_Metabolizing_Enzyme_1_Protein_Sequence | - |
| Phase_1_Metabolizing_Enzyme_1_SwissProt_ID | - |
| Phase_1_Metabolizing_Enzyme_2_Gene_Name | - |
| Phase_1_Metabolizing_Enzyme_2_ID | - |
| Phase_1_Metabolizing_Enzyme_2_Name | - |
| Phase_1_Metabolizing_Enzyme_2_Protein_Sequence | - |
| Phase_1_Metabolizing_Enzyme_2_SwissProt_ID | - |
| Phase_1_Metabolizing_Enzyme_3_Gene_Name | - |
| Phase_1_Metabolizing_Enzyme_3_ID | - |
| Phase_1_Metabolizing_Enzyme_3_Name | - |
| Phase_1_Metabolizing_Enzyme_3_Protein_Sequence | - |
| Phase_1_Metabolizing_Enzyme_3_SwissProt_ID | - |