Kisspeptins (KPs) encoded by the KiSS-1 gene are C-terminally amidated peptide products, including KP-10, KP-13, KP-14 and KP-54, which are endogenous agonists for the G-protein coupled receptor-54 (GPR54).Functional analyses have demonstrated fundamental roles of KiSS-1 in whole body homeostasis including sexualdifferentiation of brain, action on sex steroids and metabolic regulation of fertility essential for human pubertyand maintenance of adult reproduction. In addition, intensive recent investigations have provided substantialevidence suggesting roles of Kisspeptin signalling via its receptor GPR54 in the suppression of metastasis witha variety of cancers. The present review highlights the latest studies regarding the role of Kisspeptins and theKiSS-1 gene in tumor progression and also suggests targeting the KiSS-1/GPR54 system may represent a noveltherapeutic approach for cancers. Further investigations are essential to elucidate the complex pathways regulatedby the Kisspeptins and how these pathways might be involved in the suppression of metastasis across a rangeof cancers.
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