Target Information

Target General Infomation
Target ID
T39123
Former ID
TTDC00231
Target Name
G-protein coupled receptor 54
Gene Name
KISS1R
Synonyms
GPR54; KiSS-1 receptor GPR54; KISS1R
Target Type
Discontinued
Disease Prostate cancer [ICD9: 185; ICD10: C61]
Function
Receptor for metastin(kisspeptin-54 or kp-54), a C- terminally amidated peptide of KiSS1. KiSS1 is a metastasis suppressor protein that suppresses metastases in malignant melanomas and in some breast carcinomas without affecting tumorigenicity. The metastasis suppressor properties may be mediated in part by cell cycle arrest and induction of apoptosis in malignant cells. The receptor is essential for normal gonadotropin-released hormone physiology and for puberty. The hypothalamic KiSS1/KISS1R system is a pivotal factor in central regulation of the gonadotropic axis at puberty and in adulthood. The receptor is also probably involved in the regulation and fine- tuning of trophoblast invasion generated by the trophoblast itself. Analysis of the transduction pathways activated by the receptor identifies couplingto phospholipase C and intracellular calcium release through pertussis toxin-insensitive G(q) proteins.
BioChemical Class
GPCR rhodopsin
Target Validation
T39123
UniProt ID
Q969F8
Sequence
MHTVATSGPNASWGAPANASGCPGCGANASDGPVPSPRAVDAWLVPLFFAALMLLGLVGN
SLVIYVICRHKPMRTVTNFYIANLAATDVTFLLCCVPFTALLYPLPGWVLGDFMCKFVNY
IQQVSVQATCATLTAMSVDRWYVTVFPLRALHRRTPRLALAVSLSIWVGSAAVSAPVLAL
HRLSPGPRAYCSEAFPSRALERAFALYNLLALYLLPLLATCACYAAMLRHLGRVAVRPAP
ADSALQGQVLAERAGAVRAKVSRLVAAVVLLFAACWGPIQLFLVLQALGPAGSWHPRSYA
AYALKTWAHCMSYSNSALNPLLYAFLGSHFRQAFRRVCPCAPRRPRRPRRPGPSDPAAPH
AELLRLGSHPAPARAQKPGSSGLAARGLCVLGEDNAPL
Drugs and Mode of Action
Drug(s) TAK-683 Drug Info Discontinued in Phase 1 Prostate cancer [548739]
TAK-683 Drug Info Terminated Prostate cancer [548739]
Inhibitor 4-fluorobenzoyl-Phe-Gly-Leu-Arg-Trp-NH2 Drug Info [529804]
H-Tyr-Asn-Trp-Asn-Ser-Phe-Gly-Leu-Arg-Phe-NH2 Drug Info [529804]
Agonist kisspeptin-10 Drug Info [526101]
TAK-683 Drug Info [551155], [551717]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Neuroactive ligand-receptor interaction
Reactome Peptide ligand-binding receptors
G alpha (q) signalling events
WikiPathways Gastrin-CREB signalling pathway via PKC and MAPK
GPCR ligand binding
GPCR downstream signaling
References
Ref 548739Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028256)
Ref 526101The metastasis suppressor gene KiSS-1 encodes kisspeptins, the natural ligands of the orphan G protein-coupled receptor GPR54. J Biol Chem. 2001 Sep 14;276(37):34631-6. Epub 2001 Jul 16.
Ref 529804J Med Chem. 2008 Dec 11;51(23):7645-9.Development of novel G-protein-coupled receptor 54 agonists with resistance to degradation by matrix metalloproteinase.
Ref 551155The efficacy and tolerability of two novel H(1)/H(3) receptor antagonists in seasonal allergic rhinitis. Int Arch Allergy Immunol. 2012;158(1):84-98.
Ref 551717Clinical pipeline report, company report or official report of Takeda (2009).

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