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Current Protein & Peptide Science

Editor-in-Chief

ISSN (Print): 1389-2037
ISSN (Online): 1875-5550

Review Article

Pt(IV) Prodrug Photoactivation: A Promising Strategy for Cancer Therapy

Author(s): Lingkai Tang, Yafei Luo, Wenqin Luo, Guangzhou Sun, Yu Jiang, Zhigang Zhang, Xinru Yue, Siyao Li, Li Liang, Wei Liu* and Jianping Hu*

Volume 25, Issue 10, 2024

Published on: 25 June, 2024

Page: [797 - 813] Pages: 17

DOI: 10.2174/0113892037297416240525155628

Price: $65

Abstract

Platinum (II) drugs, including cisplatin, carboplatin, and oxaliplatin, have achieved significant clinical success in cancer treatment. However, their clinical application has been greatly hindered by various adverse factors, such as non-specific activation and drug resistance. Compared with Pt(II) drugs, the axial ligands within Pt(IV) compounds can improve the pharmacokinetic properties, selectivity, and biological activity, implementing alternative cytotoxic mechanisms beyond DNA cross-linking and partially overcoming drug resistance. The controlled conversion of Pt(IV) prodrugs into Pt(II) agents at the tumor site has been extensively explored internationally. In this review, Pt(IV) prodrug modification strategies are first summarized, and the development of the predominant external and internal photosensitizers is listed. Finally, three representative photoreduction mechanisms and strategies for developing corresponding Pt(IV) prodrugs are discussed. This work provides constructive instruction for the subsequent molecular design of Pt(IV) prodrugs.

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