Design and implication of a breast cancer-targeted drug delivery system utilizing the Kisspeptin/GPR54 system.
Nie. Yaoyan Y; Wei. Yanzhu Y; Zhang. Yuhuan Y; Liang. Zhuansheng Z; Lei. Zelin Z; Chang. Min M; Peng. Yali Y
Key Findings
- GPR54 receptors are over‑expressed in breast cancer cells.
- Liposomal doxorubicin coated with Kp‑10 (228‑K3‑EG8‑Liposome) shows enhanced tumor targeting in vitro and in vivo.
- Mice treated with the targeted liposomes lived significantly longer than those receiving standard liposomes or free doxorubicin.
Practical Outcomes
- For the biohacker community, this research does not translate into actionable self‑experimentation or health‑optimizing protocols. It is a pre‑clinical cancer therapy concept, and the peptide is used solely as a targeting tool rather than a supplement or performance enhancer.
Summary
Researchers attached a short kisspeptin peptide (Kp-10) to liposomes carrying the chemotherapy drug doxorubicin, aiming to target breast cancer cells that have high levels of the GPR54 receptor. In mice, these targeted liposomes accumulated more in tumors and improved survival compared to non‑targeted liposomes or free drug. The study shows a new way to deliver cancer drugs, but it does not provide any direct advice or protocols for personal health optimization.
Abstract
Kisspeptins function as endogenous ligands for the G protein-coupled receptor GPR54. While the primary role of the Kisspeptin/GPR54 signaling pathway pertains to reproduction, several studies have shown that GPR54 is highly expressed in breast cancer, and we further confirmed this result that GPR54 expression is significantly upregulated in breast cancer cells. Based on this finding, we developed a liposomal drug delivery system utilizing the Kisspeptin/GPR54 system to treat breast cancer after confirming the safety of Kp-10-228. By surface-modifying liposomes with Kp-10-228 (228-K<sub>3</sub>-EG<sub>8</sub>-Liposome), we demonstrated enhanced accumulation of these liposomes in tumor cells, both in vitro and in vivo. Doxorubicin-loaded 228-K<sub>3</sub>-EG<sub>8</sub>-Liposome exhibited a remarkable inhibition of cancer cell proliferation, significantly extending the median survival time in mice with breast tumors compared to model mice treated with non-targeted liposomes or free doxorubicin. Our results suggest that the liposomal drug delivery system utilizing the Kisspeptin/GPR54 system is a promising novel strategy for the management of breast cancer.
Study Information
pubmed
2025
2025-01-02T00:00:00.000Z
10.1016/j.ijpharm.2024.125154
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