Scientific Reference
Kisspeptin
Evidence profile: Predominantly preclinical
Kisspeptin-10 is a ten-residue peptide amide, the shortest active member of the kisspeptin family encoded by the KISS1 gene. The gene's 145-residue precursor is processed into kisspeptins of 54, 14, 13 and 10 amino acids, which all share the same C-terminal ten residues ending in Arg-Phe-NH2. Research interest in its reproductive role grew after human genetic studies linked loss of kisspeptin receptor function to a failure to enter puberty. It has since been examined in cell and animal models of hypothalamic reproductive control, and in short human physiological studies that measured gonadotropin release. Longer-term human data are limited.
Mechanism of Action
Kisspeptin-10 has been reported to bind KISS1R, also called GPR54, a G protein-coupled receptor that signals mainly through Gq/11, phospholipase C and intracellular calcium. KISS1R is expressed on gonadotropin-releasing hormone (GnRH) neurons, and kisspeptin signalling is regarded as a principal upstream input controlling their activity. In animal and human physiological studies, exposure has been followed by GnRH release and, downstream, secretion of LH and to a lesser degree FSH from the anterior pituitary. Continuous exposure has been reported in some models to desensitise the receptor, a phenomenon that is itself a topic of study.
Molecular Information
- Type: Decapeptide (KISS1-derived)
- Length: 10 amino acids
- Molecular weight: 1302.4 g/mol
- Molecular formula: C63H83N17O14