Classification of the kisspeptin receptor

Previous namesGPR54, AXOR12, hOT7T175
Structural information7TM
    Human398 aa (SwissProt Q969F8) chr. 19p13.3 (Entrez 84634)
    Rat396 aa (SwissProt Q924U1) chr. 7q11 (Entrez 78976)
    Mouse396 aa (SwissProt Q91V45) chr. 10C1 (Entrez 114229)
Functional assaysCHO cells transfected with the kisspeptin receptorHori et al., 2001
In vitro pharmacology using human isolated vesselsMead et al., 2007b
Endogenous agonistsKP-54 (EC50 = 5.5 nM)Kotani et al., 2001
KP-54 (pEC50 = 8.9 nM)Mead et al., 2007b
Selective agonists4-fluorobenzoyl-F-G-l-RW-NH2 (EC50 = 0.7 nM)Tomita et al., 2007
[dY]1KP-10Curtis et al., 2010
AntagonistsPeptide234 ac[(D)-A]NWNGFG[(D)-W]RFRoseweir et al., 2009
Antagonist potenciesPeptide 234 (IC50 = 7.0 nM)
Radioligands125I-Tyr45-KP-54 (KD = 0.1 nM)Ohtaki et al., 2001
125I-KP-14 (KD = 0.1 nM)Mead et al., 2007b
125I-KP-10 (KD = 1.9 nM)Kotani et al., 2001
Transduction mechanismsCoupled to Gαq/11 proteinsKotani et al., 2001; Muir et al., 2001; Becker et al., 2005
Receptor distribution
    HumanRT-PCR showed highest expression of KISS1R mRNA in placenta, pituitary, spinal cord and pancreas.Kotani et al., 2001; Ohtaki et al., 2001.
Kisspeptin receptor protein expression detected in the cerebral cortex, thalamus, pons-medulla and cerebellum by immunohistochemistry.Muir et al., 2001
Radioligand binding and immunohistochemistry found expression in aorta, coronary artery and umbilical vein.Mead et al., 2007b
    RatRT-PCR detected Kiss1r mRNA in cortex, frontal cortex and striatum and in ovary.Lee et al., 1999; Castellano et al., 2006
Kisspeptin-receptor immunoreactivity has been detected in the pituitary.Richard et al., 2008
    MouseRT-PCR showed Kiss1r expression in heart and in brain and reproductive tissues (uterus, oviduct, and testis).Stafford et al., 2002; Funes et al., 2003
Tissue functionMetastasis inhibitor, stimulator of LH release, inhibitor of trophoblast migration, vasoconstrictor of coronary artery, and umbilical vein.Ringel et al., 2002; Bilban et al., 2004; Irwig et al., 2004; Navarro et al., 2004a; Mead et al., 2007b
  • aa, amino acid(s); RT-PCR, reverse transcription-polymerase chain reaction.