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Updated: Feb 11, 2026

BioMEMS and Cellular Biology: Perspectives and Applications
Published on: October 1, 2007
Kisspeptin and Cancer: Molecular Interaction, Biological Functions, and Future Perspectives
Vincenza Ciaramella1, Carminia Maria Della Corte1, Fortunato Ciardiello1
1Medical Oncology, University of Campania "Luigi Vanvitelli", Naples, Italy.
Abstract:
Cancer disease is the second leading cause of death in the world and one of the main fields of medical research. Although there is now a greater understanding of biological mechanisms of uncontrolled cell growth, invasiveness and metastasization, the multi-step process of cancer development and evolution is still incompletely understood. The inhibition of molecules activated in cancer metastasization is an hot topic in cancer research. Among the known antimetastatic genes, KiSS-1 is involved in the metastatic cascade by preventing growth of metastasis. Moreover, loss of KiSS-1 protein expression by tumor cells has been associated with a more aggressive phenotype. KiSS-1 gene encodes a 145-amino acid protein, which following proteolytic cleavage, generates a family of kisspeptins (Kp-10, -13, and -14), that are endogenous agonists for the G-protein-coupled receptor (GPR54). The antitumor effect of KiSS-1 was primarily associated with the inhibition of proliferation, migration and cell invasion and, consequently, the reduced formation of metastasis and intratumoral microvessels. In this review, we highlight the latest data on the role of kisspeptin signaling in the suppression of metastasis in various cancer types and the use modulators of KiSS/GPR54 signaling as potential novel therapeutic agents for the treatment of cancer.
Insights
The KiSS-1 gene and its derived kisspeptins show potential in suppressing cancer metastasis. Modulating KiSS/GPR54 signaling may offer novel therapeutic strategies for cancer treatment.
Area of Science:
- Oncology
- Molecular Biology
- Genetics
Background:
- Cancer is a leading cause of death globally, with metastasis being a critical factor.
- Understanding cancer development and metastasis mechanisms is crucial for effective treatment.
- The KiSS-1 gene and its protein products play a role in inhibiting cancer metastasis.
Purpose of the Study:
- To review the latest findings on kisspeptin signaling in suppressing metastasis across various cancer types.
- To explore the therapeutic potential of KiSS/GPR54 signaling modulators in cancer treatment.
Main Methods:
- Literature review of studies investigating KiSS-1, kisspeptins, and GPR54 in cancer metastasis.
- Analysis of data on the role of kisspeptin signaling in inhibiting tumor cell proliferation, migration, and invasion.
- Evaluation of the impact on metastasis and angiogenesis.
Main Results:
- Loss of KiSS-1 expression correlates with increased tumor aggressiveness and metastatic potential.
- Kisspeptins, derived from the KiSS-1 gene, act as agonists for GPR54.
- KiSS-1 signaling inhibits cancer cell proliferation, migration, invasion, metastasis, and angiogenesis.
Conclusions:
- Kisspeptin signaling is a key suppressor of metastasis in multiple cancer types.
- Modulators of the KiSS/GPR54 pathway represent promising therapeutic agents for cancer treatment.
- Targeting this pathway could lead to novel anti-cancer strategies.
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