TARGETID

T39123

FORMERID

TTDC00231

UNIPROID

KISSR_HUMAN

TARGNAME

G-protein coupled receptor 54 (KISS1R)

GENENAME

KISS1R

TARGTYPE

Discontinued target

SYNONYMS

KiSS-1 receptor GPR54; KISS1R; GPR54

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.

BIOCLASS

GPCR rhodopsin

SEQUENCE

MHTVATSGPNASWGAPANASGCPGCGANASDGPVPSPRAVDAWLVPLFFAALMLLGLVGNSLVIYVICRHKPMRTVTNFYIANLAATDVTFLLCCVPFTALLYPLPGWVLGDFMCKFVNYIQQVSVQATCATLTAMSVDRWYVTVFPLRALHRRTPRLALAVSLSIWVGSAAVSAPVLALHRLSPGPRAYCSEAFPSRALERAFALYNLLALYLLPLLATCACYAAMLRHLGRVAVRPAPADSALQGQVLAERAGAVRAKVSRLVAAVVLLFAACWGPIQLFLVLQALGPAGSWHPRSYAAYALKTWAHCMSYSNSALNPLLYAFLGSHFRQAFRRVCPCAPRRPRRPRRPGPSDPAAPHAELLRLGSHPAPARAQKPGSSGLAARGLCVLGEDNAPL

DRUGINFO

TAK-683

DRUGINFO

4-fluorobenzoyl-Phe-Gly-Leu-Arg-Trp-NH2

DRUGINFO

kisspeptin-10

KEGGPATH

hsa04080:Neuroactive ligand-receptor interaction

WIKIPATH

WP1824:GPCR downstream signaling

WIKIPATH

WP1825:GPCR ligand binding

WIKIPATH

WP2664:Gastrin-CREB signalling pathway via PKC and MAPK

REACPATH

R-HSA-375276:Peptide ligand-binding receptors

REACPATH

R-HSA-416476:G alpha (q) signalling events