TABLE 3.
Classification of the kisspeptin receptor
| Previous names | GPR54, AXOR12, hOT7T175 | |
| Structural information | 7TM | |
| Human | 398 aa (SwissProt Q969F8) chr. 19p13.3 (Entrez 84634) | |
| Rat | 396 aa (SwissProt Q924U1) chr. 7q11 (Entrez 78976) | |
| Mouse | 396 aa (SwissProt Q91V45) chr. 10C1 (Entrez 114229) | |
| Functional assays | CHO cells transfected with the kisspeptin receptor | Hori et al., 2001 |
| In vitro pharmacology using human isolated vessels | Mead et al., 2007b | |
| Endogenous agonists | KP-54 (EC50 = 5.5 nM) | Kotani et al., 2001 |
| KP-54 (pEC50 = 8.9 nM) | Mead et al., 2007b | |
| Selective agonists | 4-fluorobenzoyl-F-G-l-RW-NH2 (EC50 = 0.7 nM) | Tomita et al., 2007 |
| [dY]1KP-10 | Curtis et al., 2010 | |
| Antagonists | Peptide234 ac[(D)-A]NWNGFG[(D)-W]RF | Roseweir et al., 2009 |
| Antagonist potencies | Peptide 234 (IC50 = 7.0 nM) | |
| Radioligands | 125I-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 mechanisms | Coupled to Gαq/11 proteins | Kotani et al., 2001; Muir et al., 2001; Becker et al., 2005 |
| Receptor distribution | ||
| Human | RT-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 | |
| Rat | RT-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 | |
| Mouse | RT-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 function | Metastasis 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.