Target Information

Target General Infomation
Target ID
T79473
Former ID
TTDS00254
Target Name
Lutropin-choriogonadotropic hormone receptor
Gene Name
LHCGR
Synonyms
LH/CG-R; LHR; LHRH receptor; LSH-R; Luteinizing hormone receptor; Luteinizing hormone-releasing hormone receptor; LHCGR
Target Type
Successful
Disease Breast cancer [ICD9: 174, 175; ICD10: C50]
Cancer [ICD9: 140-229; ICD10: C00-C96]
Female infertility [ICD9: 628; ICD10: N97.0]
Fertility [ICD10: N00-N99]
Heart disease [ICD9: 390-429; ICD10: I00-I52]
Infertility [ICD9: 628; ICD10: N97.0]
Leukemia [ICD9: 208.9; ICD10: C90-C95]
Myelodysplastic syndrome [ICD9: 238.7; ICD10: D46]
Function
Receptor for lutropin-choriogonadotropic hormone. The activity of this receptor is mediated by G proteins which activate adenylate cyclase.
BioChemical Class
GPCR rhodopsin
UniProt ID
P22888
Sequence
MKQRFSALQLLKLLLLLQPPLPRALREALCPEPCNCVPDGALRCPGPTAGLTRLSLAYLP
VKVIPSQAFRGLNEVIKIEISQIDSLERIEANAFDNLLNLSEILIQNTKNLRYIEPGAFI
NLPRLKYLSICNTGIRKFPDVTKVFSSESNFILEICDNLHITTIPGNAFQGMNNESVTLK
LYGNGFEEVQSHAFNGTTLTSLELKENVHLEKMHNGAFRGATGPKTLDISSTKLQALPSY
GLESIQRLIATSSYSLKKLPSRETFVNLLEATLTYPSHCCAFRNLPTKEQNFSHSISENF
SKQCESTVRKVNNKTLYSSMLAESELSGWDYEYGFCLPKTPRCAPEPDAFNPCEDIMGYD
FLRVLIWLINILAIMGNMTVLFVLLTSRYKLTVPRFLMCNLSFADFCMGLYLLLIASVDS
QTKGQYYNHAIDWQTGSGCSTAGFFTVFASELSVYTLTVITLERWHTITYAIHLDQKLRL
RHAILIMLGGWLFSSLIAMLPLVGVSNYMKVSICFPMDVETTLSQVYILTILILNVVAFF
IICACYIKIYFAVRNPELMATNKDTKIAKKMAILIFTDFTCMAPISFFAISAAFKVPLIT
VTNSKVLLVLFYPINSCANPFLYAIFTKTFQRDFFLLLSKFGCCKRRAELYRRKDFSAYT
SNCKNGFTGSNKPSQSTLKLSTLHCQGTALLDKTRYTEC
Drugs and Mode of Action
Drug(s) Choriogonadotropin alfa Drug Info Approved Female infertility [536361]
Gonadotropin, Chorionic Drug Info Approved Fertility [551871]
Lutropin alfa Drug Info Approved Female infertility [536361]
ML-04 Drug Info Phase 2 Myelodysplastic syndrome [521530]
Org-43902 Drug Info Phase 1 Infertility [549583]
LDI-200 Drug Info Discontinued in Phase 3 Leukemia [546170]
Human chorionic gonadotropin Drug Info Terminated Heart disease [538686], [546721]
Modulator Choriogonadotropin alfa Drug Info [556264]
EP-200 Drug Info [543644]
Gonadotropin, Chorionic Drug Info [556264]
LDI-200 Drug Info [543644]
ML-04 Drug Info [528609]
Inhibitor Human chorionic gonadotropin Drug Info [543644]
Agonist Labeled LH superagonist Drug Info [543644]
LH superagonists Drug Info [543644]
Org-43902 Drug Info [532276]
Binder Lutropin alfa Drug Info [536778]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Calcium signaling pathway
Neuroactive ligand-receptor interaction
Ovarian steroidogenesis
Prolactin signaling pathway
NetPath Pathway FSH Signaling Pathway
Pathway Interaction Database Arf6 signaling events
PathWhiz Pathway Intracellular Signalling Through LHCGR Receptor and Luteinizing Hormone/Choriogonadotropin
Reactome Hormone ligand-binding receptors
G alpha (s) signalling events
WikiPathways GPCRs, Class A Rhodopsin-like
Ovarian Infertility Genes
Peptide GPCRs
GPCR ligand binding
GPCR downstream signaling
References
Ref 521530ClinicalTrials.gov (NCT00044226) A 20-Week Study of a New Treatment for Men With Benign Prostatic Hyperplasia (BPH).. U.S. National Institutes of Health.
Ref 536361Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20.
Ref 538686(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: 1160).
Ref 546170Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006739)
Ref 546721Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009926)
Ref 549583Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800042073)
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 528609Evaluation of radiolabeled ML04, a putative irreversible inhibitor of epidermal growth factor receptor, as a bioprobe for PET imaging of EGFR-overexpressing tumors. Nucl Med Biol. 2007 Jan;34(1):55-70.
Ref 532276First evidence of ovulation induced by oral LH agonists in healthy female volunteers of reproductive age. J Clin Endocrinol Metab. 2013 Apr;98(4):1558-66.
Ref 536778Lutropin alfa. Drugs. 2008;68(11):1529-40.
Ref 543644(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: 254).
Ref 556264Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.

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