The KiSS-1/GPR54 system: Essential roles in physiological homeostasis and cancer biology

KiSS-1, first identified as an anti-metastasis gene in melanoma, encodes C-terminally amidated peptide products, including kisspeptin-145, kisspeptin-54, kisspeptin-14, kisspeptin-13 and kisspeptin-10. These products are endogenous ligands coupled to G proteincoupled receptor 54 (GPR54)/h0T7T175/AX0R12. To date, the regulatory activities of the KiSS-1/GPR54 system, such as puberty initiation, antitumor metastasis, fertility in adulthood, hypothalamic-pituitary-gonadal axis (HPG axis) feedback, and trophoblast invasion, have been investigated intensively. Accumulating evidence has demonstrated that KiSS-1 played a key role in reproduction and served as a promising biomarker relative to the diagnosis, identification of therapeutic targets and prognosis in various carcinomas, while few studies have systematically summarized its subjective factors and concluded the functions of KiSS-1/GPR54 signaling in physiology homeostasis and cancer biology. In this review, we retrospectively summarized the regulators of the KiSS-1/GPR54 system in different animal models and reviewed its functions according to physiological homeostasis regulations and above all, cancer biology, which provided us with a profound understanding of applying the KiSS-1/GPR54 system into medical applications. Copyright (C) 2020, Chongqing Medical University. Production and hosting by Elsevier B.V.

Automated summary

KiSS-1 is an anti-metastasis gene encoding peptide products that act as endogenous ligands for G proteincoupled receptor 54, regulating various physiological activities such as puberty initiation, fertility, and feedback in the HPG axis. It plays a crucial role in cancer biology, serving as a promising biomarker for diagnosis, therapeutic target identification, and prognosis.