Target Information
Target General Information | Top | |||||
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Target ID |
T12475
(Former ID: TTDS00273)
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Target Name |
Gonadotropin-releasing hormone receptor (GNRHR)
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Synonyms |
Hypothalamic gonadotropin-releasing hormone receptor; Gonadotrophin releasing hormone receptor; GnRH-R; GnRH receptor; GRHR
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Gene Name |
GNRHR
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Target Type |
Successful target
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[1] | ||||
Disease | [+] 6 Target-related Diseases | + | ||||
1 | Endometriosis [ICD-11: GA10] | |||||
2 | Ovarian developmental anomaly [ICD-11: LB45] | |||||
3 | Ovarian dysfunction [ICD-11: 5A80] | |||||
4 | Pituitary gland disorder [ICD-11: 5A60-5A61] | |||||
5 | Prostate cancer [ICD-11: 2C82] | |||||
6 | Solid tumour/cancer [ICD-11: 2A00-2F9Z] | |||||
Function |
Receptor for gonadotropin releasing hormone (GnRH) that mediates the action of GnRH to stimulate the secretion of the gonadotropic hormones luteinizing hormone (LH) and follicle-stimulating hormone (FSH). This receptor mediates its action by association with G-proteins that activate a phosphatidylinositol-calcium second messenger system. Isoform 2 may act as an inhibitor of GnRH-R signaling.
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BioChemical Class |
GPCR rhodopsin
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UniProt ID | ||||||
Sequence |
MANSASPEQNQNHCSAINNSIPLMQGNLPTLTLSGKIRVTVTFFLFLLSATFNASFLLKL
QKWTQKKEKGKKLSRMKLLLKHLTLANLLETLIVMPLDGMWNITVQWYAGELLCKVLSYL KLFSMYAPAFMMVVISLDRSLAITRPLALKSNSKVGQSMVGLAWILSSVFAGPQLYIFRM IHLADSSGQTKVFSQCVTHCSFSQWWHQAFYNFFTFSCLFIIPLFIMLICNAKIIFTLTR VLHQDPHELQLNQSKNNIPRARLKTLKMTVAFATSFTVCWTPYYVLGIWYWFDPEMLNRL SDPVNHFFFLFAFLNPCFDPLIYGYFSL Click to Show/Hide
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3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
HIT2.0 ID | T45C0Q |
Drugs and Modes of Action | Top | |||||
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Approved Drug(s) | [+] 10 Approved Drugs | + | ||||
1 | Abarelix | Drug Info | Approved | Prostate cancer | [2], [3] | |
2 | Cetrorelix | Drug Info | Approved | Ovarian stimulation | [4], [5] | |
3 | Degarelix | Drug Info | Approved | Prostate cancer | [6], [7] | |
4 | Elagolix sodium | Drug Info | Approved | Endometriosis | [8] | |
5 | Ganirelix | Drug Info | Approved | Ovulation dysfunction | [9], [10] | |
6 | Gonadorelin | Drug Info | Approved | Hypothalamic hypogonadism | [10], [11] | |
7 | Leuprorelin acetate | Drug Info | Approved | Prostate cancer | [12] | |
8 | Nafarelin | Drug Info | Approved | Endometriosis | [10], [13] | |
9 | Relugolix | Drug Info | Approved | Prostate cancer | [14] | |
10 | Triptorelin | Drug Info | Approved | Solid tumour/cancer | [10], [15] | |
Clinical Trial Drug(s) | [+] 8 Clinical Trial Drugs | + | ||||
1 | AEZS-108 | Drug Info | Phase 3 | Acute lymphoblastic leukaemia | [16] | |
2 | Elagolix | Drug Info | Phase 3 | Uterine fibroids | [17], [18] | |
3 | GnRH | Drug Info | Phase 3 | Female infertility | [19] | |
4 | ACYLINE | Drug Info | Phase 2 | Prostate cancer | [20] | |
5 | ASP-1707 | Drug Info | Phase 2 | Endometriosis | [21] | |
6 | KLH-2109 | Drug Info | Phase 2 | Endometriosis | [22] | |
7 | Ozarelix | Drug Info | Phase 2 | Prostate disease | [23] | |
8 | PEP-223/CoVaccine HT | Drug Info | Phase 1/2 | Prostate cancer | [24] | |
Discontinued Drug(s) | [+] 9 Discontinued Drugs | + | ||||
1 | Antide | Drug Info | Discontinued in Phase 2 | Prostate hyperplasia | [25], [26] | |
2 | Gonadimmune | Drug Info | Discontinued in Phase 2 | Prostate cancer | [27] | |
3 | TAK-013 | Drug Info | Discontinued in Phase 2 | Uterine fibroids | [28], [29] | |
4 | A-75998 | Drug Info | Discontinued in Phase 1 | Hormone deficiency | [30] | |
5 | NBI-42902 | Drug Info | Discontinued in Phase 1 | Prostate cancer | [31], [32] | |
6 | Prostate cancer vaccine | Drug Info | Discontinued in Phase 1 | Prostate cancer | [33] | |
7 | Ramorelix | Drug Info | Discontinued in Phase 1 | Esophageal cancer | [34] | |
8 | D-21775 | Drug Info | Terminated | Solid tumour/cancer | [36] | |
9 | D-26344 | Drug Info | Terminated | Solid tumour/cancer | [37] | |
Preclinical Drug(s) | [+] 1 Preclinical Drugs | + | ||||
1 | 5-(N,N-hexamethylene)-amiloride | Drug Info | Preclinical | Coronavirus infection | [35] | |
Mode of Action | [+] 5 Modes of Action | + | ||||
Modulator | [+] 9 Modulator drugs | + | ||||
1 | Abarelix | Drug Info | [38] | |||
2 | Triptorelin | Drug Info | [45] | |||
3 | AEZS-108 | Drug Info | [46] | |||
4 | GnRH | Drug Info | [48] | |||
5 | Ozarelix | Drug Info | [23] | |||
6 | Gonadimmune | Drug Info | [53] | |||
7 | D-21775 | Drug Info | [48] | |||
8 | detirelix | Drug Info | [61], [62] | |||
9 | Org-30850 | Drug Info | [67] | |||
Antagonist | [+] 16 Antagonist drugs | + | ||||
1 | Cetrorelix | Drug Info | [1], [39] | |||
2 | Elagolix sodium | Drug Info | [8] | |||
3 | Ganirelix | Drug Info | [41] | |||
4 | Relugolix | Drug Info | [14] | |||
5 | Elagolix | Drug Info | [47] | |||
6 | ASP-1707 | Drug Info | [50] | |||
7 | Antide | Drug Info | [52] | |||
8 | A-75998 | Drug Info | [55] | |||
9 | Ramorelix | Drug Info | [57] | |||
10 | AEZS-115 | Drug Info | [48] | |||
11 | antarelix | Drug Info | [60] | |||
12 | FD-1 | Drug Info | [58] | |||
13 | furan-1 | Drug Info | [63] | |||
14 | IN-3 | Drug Info | [64] | |||
15 | LXT-101 | Drug Info | [66] | |||
16 | [125I]cetrorelix | Drug Info | [70] | |||
Inhibitor | [+] 44 Inhibitor drugs | + | ||||
1 | Degarelix | Drug Info | [40] | |||
2 | ACYLINE | Drug Info | [49] | |||
3 | TAK-013 | Drug Info | [54] | |||
4 | NBI-42902 | Drug Info | [56] | |||
5 | D-26344 | Drug Info | [59] | |||
6 | AN-207 | Drug Info | [48] | |||
7 | AZALINE B | Drug Info | [49] | |||
8 | LHRH | Drug Info | [65] | |||
9 | PGlu-His-Trp-Ser-His-D-Tyr-Leu-Arg-Pro-Gly-NH2 | Drug Info | [68] | |||
10 | PGlu-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly-NH2 | Drug Info | [68] | |||
11 | T-98475 | Drug Info | [54] | |||
12 | WAY-207024 | Drug Info | [69] | |||
13 | [4Aph(CO-(C2H4O)3-C2H4-NH-CO-NH-OCH3)5]degarelix | Drug Info | [71] | |||
14 | [4Aph(CO-NH-(C2H4O)2-C2H5)5]degarelix | Drug Info | [71] | |||
15 | [4Aph(CO-NH-OCH3)5,D-4Aph(CO-NH-OCH3)6]degarelix | Drug Info | [71] | |||
16 | [4Aph(CO-NH-OCH3)5]degarelix | Drug Info | [71] | |||
17 | [4Aph(CO-NH-OH)5]degarelix | Drug Info | [71] | |||
18 | [D-4Aph(CO-NH-(C2H4O)2-C2H5)6]degarelix | Drug Info | [71] | |||
19 | [D-4Aph(CO-NH-OCH3)6]degarelix | Drug Info | [71] | |||
20 | [D-4Aph(CO-NH-OH)6]degarelix | Drug Info | [71] | |||
21 | [D-Dab(CO-NH-OCH3)3]degarelix | Drug Info | [71] | |||
22 | [D-Dab(CO-NH-OH)3]degarelix | Drug Info | [71] | |||
23 | [D-Dap(CO-NH-OCH3)3]degarelix | Drug Info | [71] | |||
24 | [D-Dap(CO-NH-OH)3]degarelix | Drug Info | [71] | |||
25 | [D-Gln3,D-Ncy(isopropyl)7]acyline | Drug Info | [49] | |||
26 | [D-Gln3,D-Ncy(SO,isopropyl)7]acyline | Drug Info | [49] | |||
27 | [D-Gln3,D-Ncy(SO2,isopropyl)7]acyline | Drug Info | [49] | |||
28 | [D-Gln3,Ncy(isopropyl)7]acyline | Drug Info | [49] | |||
29 | [D-Gln3,Ncy(SO,isopropyl)7]acyline | Drug Info | [49] | |||
30 | [D-Gln3,Ncy(SO2,isopropyl)7]acyline | Drug Info | [49] | |||
31 | [D-Ncy(2-naphthyl)1]acyline | Drug Info | [49] | |||
32 | [D-Ncy(isopropyl)7]acyline | Drug Info | [49] | |||
33 | [D-Ncy(methyl)10] acyline | Drug Info | [49] | |||
34 | [D-Ncy(methyl)4]acyline | Drug Info | [49] | |||
35 | [D-Ncy(SO,isopropyl)7]acyline | Drug Info | [49] | |||
36 | [D-Ncy(SO,methyl)10]acyline | Drug Info | [49] | |||
37 | [D-Ncy(SO,methyl)4]acyline | Drug Info | [49] | |||
38 | [Ncy(2-naphthyl)1]acyline | Drug Info | [49] | |||
39 | [Ncy(isopropyl)7]acyline | Drug Info | [49] | |||
40 | [Ncy(methyl)10]acyline | Drug Info | [49] | |||
41 | [Ncy(methyl)4]acyline | Drug Info | [49] | |||
42 | [Ncy(SO,isopropyl)7]acyline | Drug Info | [49] | |||
43 | [Ncy(SO,methyl)10]acyline | Drug Info | [49] | |||
44 | [Ncy(SO,methyl)4]acyline | Drug Info | [49] | |||
Agonist | [+] 4 Agonist drugs | + | ||||
1 | Gonadorelin | Drug Info | [42] | |||
2 | Leuprorelin acetate | Drug Info | [43] | |||
3 | Nafarelin | Drug Info | [44] | |||
4 | KLH-2109 | Drug Info | [51] | |||
Modulator (allosteric modulator) | [+] 1 Modulator (allosteric modulator) drugs | + | ||||
1 | 5-(N,N-hexamethylene)-amiloride | Drug Info | [58] |
Chemical Structure based Activity Landscape of Target | Top |
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Drug Property Profile of Target | Top | |
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(1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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(5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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"RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five |
Target Poor or Non Binders | Top | |||||
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Target Poor or Non Binders |
Target Regulators | Top | |||||
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Target-regulating Transcription Factors |
Target Profiles in Patients | Top | |||||
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Target Expression Profile (TEP) |
Target Affiliated Biological Pathways | Top | |||||
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KEGG Pathway | [+] 2 KEGG Pathways | + | ||||
1 | Neuroactive ligand-receptor interaction | |||||
2 | GnRH signaling pathway | |||||
NetPath Pathway | [+] 2 NetPath Pathways | + | ||||
1 | IL1 Signaling Pathway | |||||
2 | IL2 Signaling Pathway | |||||
Panther Pathway | [+] 1 Panther Pathways | + | ||||
1 | Heterotrimeric G-protein signaling pathway-Gq alpha and Go alpha mediated pathway | |||||
Reactome | [+] 2 Reactome Pathways | + | ||||
1 | Hormone ligand-binding receptors | |||||
2 | G alpha (q) signalling events | |||||
WikiPathways | [+] 5 WikiPathways | + | ||||
1 | Gastrin-CREB signalling pathway via PKC and MAPK | |||||
2 | Peptide GPCRs | |||||
3 | GPCR ligand binding | |||||
4 | GPCR downstream signaling | |||||
5 | GPCRs, Other |
Target-Related Models and Studies | Top | |||||
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Target Validation |
References | Top | |||||
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REF 1 | Gonadotropin 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. | |||||
REF 2 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1188). | |||||
REF 3 | Abarelix for injectable suspension: first-in-class gonadotropin-releasing hormone antagonist for prostate cancer. Future Oncol. 2006 Dec;2(6):677-96. | |||||
REF 4 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1190). | |||||
REF 5 | New drugs in development for the treatment of endometriosis. Expert Opin Investig Drugs. 2008 Aug;17(8):1187-202. | |||||
REF 6 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5585). | |||||
REF 7 | ClinicalTrials.gov (NCT01512472) Firmagon (Degarelix) Intermittent Therapy. U.S. National Institutes of Health. | |||||
REF 8 | 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89. | |||||
REF 9 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 3877). | |||||
REF 10 | Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. | |||||
REF 11 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4391). | |||||
REF 12 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
REF 13 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 3902). | |||||
REF 14 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020 | |||||
REF 15 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1177). | |||||
REF 16 | ClinicalTrials.gov (NCT01767155) Study Comparing AEZS-108/ZoptEC (Zoptarelin Doxorubicin in Endometrial Cancer) to Doxorubicin as a Second Line Therapy of Endometrial Cancer. U.S. National Institutesof Health. | |||||
REF 17 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 8362). | |||||
REF 18 | ClinicalTrials.gov (NCT01620528) A Clinical Study to Evaluate the Safety and Efficacy of Elagolix in Subjects With Moderate to Severe Endometriosis-Associated Pain. U.S. National Institutes of Health. | |||||
REF 19 | Clinical pipeline report, company report or official report of Ferring Pharmaceuticals Inc. | |||||
REF 20 | ClinicalTrials.gov (NCT02147964) ITT-5 Mechanisms of Spermatogenesis. U.S. National Institutes of Health. | |||||
REF 21 | ClinicalTrials.gov (NCT01767090) A Study to Assess the Effectiveness and Safety of Different Doses of ASP1707 Compared to Placebo for Endometriosis Associated Pelvic Pain. U.S. National Institutes ofHealth. | |||||
REF 22 | ClinicalTrials.gov (NCT01533532) A Randomized, Placebo-controlled, Double-blind Study of KLH-2109 in Patients With Endometriosis (2). U.S. National Institutes of Health. | |||||
REF 23 | Ozarelix, a fourth generation GnRH antagonist, induces apoptosis in hormone refractory androgen receptor negative prostate cancer cells modulating expression and activity of death receptors. Prostate. 2010 Sep 1;70(12):1340-9. | |||||
REF 24 | ClinicalTrials.gov (NCT00895466) Efficacy and Safety Study of the Therapeutic Vaccine PEP223 in Prostate Cancer Patients. U.S. National Institutes of Health. | |||||
REF 25 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 3854). | |||||
REF 26 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000763) | |||||
REF 27 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007230) | |||||
REF 28 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1185). | |||||
REF 29 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800017215) | |||||
REF 30 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003694) | |||||
REF 31 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1178). | |||||
REF 32 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013539) | |||||
REF 33 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014087) | |||||
REF 34 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008630) | |||||
REF 35 | Coronaviruses - drug discovery and therapeutic options. Nat Rev Drug Discov. 2016 May;15(5):327-47. | |||||
REF 36 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003256) | |||||
REF 37 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013297) | |||||
REF 38 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. | |||||
REF 39 | Gonadotrophin-releasing hormone antagonists for assisted conception. Cochrane Database Syst Rev. 2006 Jul 19;3:CD001750. | |||||
REF 40 | Iterative approach to the discovery of novel degarelix analogues: substitutions at positions 3, 7, and 8. Part II. J Med Chem. 2005 Jul 28;48(15):4851-60. | |||||
REF 41 | Age attenuates testosterone secretion driven by amplitude-varying pulses of recombinant human luteinizing hormone during acute gonadotrope inhibiti... J Clin Endocrinol Metab. 2007 Sep;92(9):3626-32. | |||||
REF 42 | Use of cognitive behavior therapy for functional hypothalamic amenorrhea. Ann N Y Acad Sci. 2006 Dec;1092:114-29. | |||||
REF 43 | Clinical pipeline report, company report or official report of Takeda (2009). | |||||
REF 44 | Reversible downregulation of endocrine and germinative testicular function (hormonal castration) in the dog with the GnRH-agonist azagly-nafarelin ... Theriogenology. 2009 Apr 15;71(7):1037-45. | |||||
REF 45 | Regulation of GnRH I receptor gene expression by the GnRH agonist triptorelin, estradiol, and progesterone in the gonadotroph-derived cell line alphaT3-1. Endocrine. 2006 Aug;30(1):139-44. | |||||
REF 46 | Stability of cytotoxic luteinizing hormone-releasing hormone conjugate (AN-152) containing doxorubicin 14-O-hemiglutarate in mouse and human serum in vitro: implications for the design of preclinicalstudies. Proc Natl Acad Sci U S A. 2000 Jan 18;97(2):829-34. | |||||
REF 47 | Elagolix, a novel, orally bioavailable GnRH antagonist under investigation for the treatment of endometriosis-related pain. Womens Health (Lond Engl). 2015 Jan;11(1):19-28. | |||||
REF 48 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 256). | |||||
REF 49 | Structure-activity relationship studies of gonadotropin-releasing hormone antagonists containing S-aryl/alkyl norcysteines and their oxidized deriv... J Med Chem. 2007 May 3;50(9):2067-77. | |||||
REF 50 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800032657) | |||||
REF 51 | Clinical pipeline report, company report or official report of Avarx. | |||||
REF 52 | Antide (Nal-Lys GnRH antagonist) suppression of pituitary-testicular function and sexual behavior in group-living rhesus monkeys. Physiol Behav. 1991 Aug;50(2):429-35. | |||||
REF 53 | A novel retro-inverso gonadotropin-releasing hormone (GnRH) immunogen elicits antibodies that neutralize the activity of native GnRH. Endocrinology. 2003 Jul;144(7):3262-9. | |||||
REF 54 | Non-peptide gonadotropin-releasing hormone receptor antagonists. J Med Chem. 2008 Jun 26;51(12):3331-48. | |||||
REF 55 | Physicochemical properties of A-75998, an antagonist of luteinizing hormone releasing hormone. J Pharm Sci. 1995 Aug;84(8):953-8. | |||||
REF 56 | 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. J Med Chem. 2008 Dec 11;51(23):7478-85. | |||||
REF 57 | Effects of the luteinizing-hormone-releasing hormone (LHRH) antagonist ramorelix (hoe013) and the LHRH agonist buserelin on dimethylbenz[]anthracene-induced mammary carcinoma: studies with slow-release formulations. J Cancer Res Clin Oncol. 1993;119(8):457-62. | |||||
REF 58 | Amiloride derivatives and a nonpeptidic antagonist bind at two distinct allosteric sites in the human gonadotropin-releasing hormone receptor. Mol Pharmacol. 2008 Jun;73(6):1808-15. | |||||
REF 59 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003256) | |||||
REF 60 | Characterization of gonadotropin-releasing hormone analogs based on a sensitive cellular luciferase reporter gene assay. Anal Biochem. 1997 Aug 15;251(1):17-23. | |||||
REF 61 | Inhibition of follicular development by a potent antagonistic analog of gonadotropin-releasing hormone (detirelix). J Clin Endocrinol Metab. 1991 Apr;72(4):927-33. | |||||
REF 62 | Gonadotropin-releasing hormone receptor-targeted paclitaxel-degarelix conjugate: synthesis and in vitro evaluation.J Pept Sci.2015 Jul;21(7):569-76. | |||||
REF 63 | Biological characterization of a novel, orally active small molecule gonadotropin-releasing hormone (GnRH) antagonist using castrated and intact rats. J Pharmacol Exp Ther. 2003 May;305(2):688-95. | |||||
REF 64 | Rescue of hypogonadotropic hypogonadism-causing and manufactured GnRH receptor mutants by a specific protein-folding template: misrouted proteins as a novel disease etiology and therapeutic target. JClin Endocrinol Metab. 2002 Jul;87(7):3255-62. | |||||
REF 65 | Discovery of a novel, potent, and orally active nonpeptide antagonist of the human luteinizing hormone-releasing hormone (LHRH) receptor. J Med Chem. 1998 Oct 22;41(22):4190-5. | |||||
REF 66 | In vivo characterization of a novel GnRH (gonadotropin-releasing hormone) antagonist, LXT-101, in normal male rats. Regul Pept. 2006 Sep 11;136(1-3):122-9. | |||||
REF 67 | In vivo effects of a potent GnRH antagonist ORG 30850: physiologic evidence that down-regulation of GnRH receptors does not occur. J Soc Gynecol Investig. 1994 Oct-Dec;1(4):290-6. | |||||
REF 68 | Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. J Med Chem. 2006 Jan 26;49(2):637-47. | |||||
REF 69 | Synthesis and biological evaluation of piperazinyl heterocyclic antagonists of the gonadotropin releasing hormone (GnRH) receptor. Bioorg Med Chem Lett. 2010 Apr 15;20(8):2512-5. | |||||
REF 70 | Residues within transmembrane helices 2 and 5 of the human gonadotropin-releasing hormone receptor contribute to agonist and antagonist binding. Mol Endocrinol. 2000 Jul;14(7):1099-115. | |||||
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