Chalcoplatin, a dual-targeting and p53 activator-containing anticancer platinum(iv) prodrug with unique mode of action

Lili Ma, Rong Ma, Yiping Wang, Xiaoyue Zhu, Junliang Zhang, Hoi Ching Chan, Xianfeng Chen, Wenjun Zhang, Sung Kay Chiu, Guangyu Zhu*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

Abstract / Description of output

Complexation of cisplatin with a p53 activator as a single anticancer agent resulted in synergistically improved cytotoxicity in p53 wild-type but not p53 null human cancer cells. Mechanistic investigation was carried out on this dual-targeting Pt(iv) prodrug, chalcoplatin. The prodrug effectively entered cancer cells and arrested the cell cycle at the S and G2/M phases, distinctive of that from cisplatin. Chalcoplatin significantly induced p53 activation as well as the subsequent apoptosis pathways. This unique mode of action renders chalcoplatin remarkably cytotoxic and makes this compound among the first examples of a Pt(iv) prodrug that directly interacts with the downstream pathway after the formation of Pt-DNA lesions. This journal is

Original languageEnglish
Pages (from-to)6301-6304
Number of pages4
JournalChemical Communications
Volume51
Issue number29
DOIs
Publication statusPublished - 14 Apr 2015

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