Kisspeptins and the control of gonadotropin secretion in humans

The kisspeptin hormones are a family of peptides encoded by the KiSS-1 gene, which bind to the G-protein coupled receptor-54 (GPR54). Interactions between kisspeptin and GPR54 are thought to play a critical role in reproduction. In agreement with animal data, kisspeptin-54 administration acutely stimulates the release of gonadotrophins in both male and female healthy subjects, with no observed adverse effects. Furthermore, its potency is comparable to those of other gonadotrophin secretagogues studied. The kisspeptin-GPR54 system thus offers a novel means of therapeutically manipulating the hypothalamo-pituitary-gonadal (HPG) axis in humans. This article aims to provide a focused review of the experimental data which inform us how kisspeptin influences the HPG axis in humans.