Target Information

Target General Infomation
Target ID
T68334
Former ID
TTDS00438
Target Name
Follicle stimulating hormone receptor
Gene Name
FSHR
Synonyms
FSH-R; Follitropin receptor; FSHR
Target Type
Successful
Disease African trypanosomiasis [ICD9: 86.5; ICD10: B56]
Contraception [ICD10: Z30]
Female infertility [ICD9: 628; ICD10: N97.0]
Ovarian cancer [ICD9: 183; ICD10: C56]
Function
Receptor for follicle stimulating hormone. The activity of this receptor is mediated by G proteins which activate adenylate cyclase.
BioChemical Class
GPCR rhodopsin
Target Validation
T68334
UniProt ID
P23945
Sequence
MALLLVSLLAFLSLGSGCHHRICHCSNRVFLCQESKVTEIPSDLPRNAIELRFVLTKLRV
IQKGAFSGFGDLEKIEISQNDVLEVIEADVFSNLPKLHEIRIEKANNLLYINPEAFQNLP
NLQYLLISNTGIKHLPDVHKIHSLQKVLLDIQDNINIHTIERNSFVGLSFESVILWLNKN
GIQEIHNCAFNGTQLDELNLSDNNNLEELPNDVFHGASGPVILDISRTRIHSLPSYGLEN
LKKLRARSTYNLKKLPTLEKLVALMEASLTYPSHCCAFANWRRQISELHPICNKSILRQE
VDYMTQARGQRSSLAEDNESSYSRGFDMTYTEFDYDLCNEVVDVTCSPKPDAFNPCEDIM
GYNILRVLIWFISILAITGNIIVLVILTTSQYKLTVPRFLMCNLAFADLCIGIYLLLIAS
VDIHTKSQYHNYAIDWQTGAGCDAAGFFTVFASELSVYTLTAITLERWHTITHAMQLDCK
VQLRHAASVMVMGWIFAFAAALFPIFGISSYMKVSICLPMDIDSPLSQLYVMSLLVLNVL
AFVVICGCYIHIYLTVRNPNIVSSSSDTRIAKRMAMLIFTDFLCMAPISFFAISASLKVP
LITVSKAKILLVLFHPINSCANPFLYAIFTKNFRRDFFILLSKCGCYEMQAQIYRTETSS
TVHNTHPRNGHCSSAPRVTNGSTYILVPLSHLAQN
Drugs and Mode of Action
Drug(s) Follitropin beta Drug Info Approved Female infertility [536361]
Menotropins Drug Info Approved Female infertility [538545]
Urofollitropin Drug Info Approved Female infertility [536361]
Suramin Drug Info Phase 1 African trypanosomiasis [536135], [539079]
Binder Follitropin beta Drug Info [536881]
Menotropins Drug Info [537880]
Urofollitropin Drug Info [536117]
Modulator FSHR NAM Drug Info [543643]
Long-acting FSH conjugate Drug Info [543643]
PRX-111 Drug Info [534648]
Recombinant follicle stimulating hormone Drug Info [543643]
Agonist Labeled FSH superagonist Drug Info [543643]
Antagonist Suramin Drug Info [536432], [536924]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway cAMP signaling pathway
Neuroactive ligand-receptor interaction
Ovarian steroidogenesis
PathWhiz Pathway Vasopressin Regulation of Water Homeostasis
Intracellular Signalling Through FSH Receptor and Follicle Stimulating Hormone
Reactome Hormone ligand-binding receptors
G alpha (s) signalling events
WikiPathways GPCRs, Class A Rhodopsin-like
Ovarian Infertility Genes
Peptide GPCRs
FSH signaling pathway
GPCR ligand binding
GPCR downstream signaling
GPCRs, Other
References
Ref 536135Opportunities and challenges in antiparasitic drug discovery. Nat Rev Drug Discov. 2005 Sep;4(9):727-40.
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 538545FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 020328.
Ref 539079(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: 1728).
Ref 534648A naturally occurring basically charged human follicle-stimulating hormone (FSH) variant inhibits FSH-induced androgen aromatization and tissue-type plasminogen activator enzyme activity in vitro. Neuroendocrinology. 1998 Mar;67(3):153-63.
Ref 536117Follicle-stimulating hormone in clinical practice: an update. Treat Endocrinol. 2004;3(3):161-71.
Ref 536432Follicle stimulating hormone receptor (FSHR) antagonist and epithelial ovarian cancer (EOC). J Exp Ther Oncol. 2007;6(3):201-4.
Ref 536881Follitropin-alpha (Gonal-F) versus follitropin-beta (Puregon) in controlled ovarian hyperstimulation for in vitro fertilization: is there any difference? Fertil Steril. 2009 Apr;91(4 Suppl):1522-5. Epub 2008 Oct 11.
Ref 536924Suramin: clinical uses and structure-activity relationships. Mini Rev Med Chem. 2008 Nov;8(13):1384-94.
Ref 537880The role of gonadotropins in ovulation induction. Am J Obstet Gynecol. 1995 Feb;172(2 Pt 2):759-65.
Ref 543643(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: 253).

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