Zhu, Y; Zhang, M; Luo, L; Gill, MR; De Pace, C; Battaglia, G; Zhang, Q; ... Tian, X; + view all Zhu, Y; Zhang, M; Luo, L; Gill, MR; De Pace, C; Battaglia, G; Zhang, Q; Zhou, H; Wu, J; Tian, Y; Tian, X; - view fewer (2019) NF-κB hijacking theranostic Pt(ll) complex in cancer therapy. Theranostics , 9 (8) pp. 2158-2166. 10.7150/thno.30886.

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Abstract

Platinum complexes have been used for anti-cancer propose for decades, however, their high side effects resulting from damage to healthy cells cannot be neglected and prevent further clinical utilisation. Here, we designed a cyclometalated platinum (II) complex that can bind the endogenous nuclear factor-κB (NF-κB) protein. Employing detailed colocalization studies in co-culture cell line models, we show that by binding to NF-κB, the platinum (II) complex is capable of upregulated nuclear translocation specifically in cancer but not normal cells, thereby impairing cancer proliferation without disturbing healthy cells. In a murine tumour model, the platinum (II) complex prevents tumour growth to a greater extent than cisplatin and with considerably lower side-effects and kidney damage. Considering its weak damage to normal cells combined with high toxicity to cancer cells, this NF-κB-binding platinum complex is a potential anti-cancer candidate and acts to verify the strategy of hijacking endogenous trans-nuclear proteins to achieve cancer-cell specificity and enhance therapeutic indices.

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