Current Protein & Peptide ScienceCurrent Protein & Peptide ScienceCurrent Protein & Peptide Science1389-20371875-5550Bentham Science64542910.2174/0113892037297416240525155628Life SciencesResearch ArticlePt(IV) Prodrug Photoactivation: A Promising Strategy for Cancer TherapyTangLingkaiinfo@benthamscience.netLuoYafeiinfo@benthamscience.netLuoWenqininfo@benthamscience.netSunGuangzhouinfo@benthamscience.netJiangYuinfo@benthamscience.netZhangZhiganginfo@benthamscience.netYueXinruinfo@benthamscience.netLiSiyaoinfo@benthamscience.netLiangLiinfo@benthamscience.netLiuWeiinfo@benthamscience.netHuJianpinginfo@benthamscience.netKey Laboratory of Medicinal and Edible Plants Resources Development of Sichuan Education Department, School of Pharmacy, Chengdu UniversityCollaborative Innovation Center of Targeted Therapeutics and Innovation, Chongqing Key Laboratory of Kinase Modulators As Innovative Medicine, Chongqing Engineering Laboratory of Targeted and Innovative Therapeutics, International Academy of Targeted Therapeutics and Innovation,, Chongqing University of Arts and Sciences,Key Laboratory of Medicinal and Edible Plants Resources Development of Sichuan Education Department, School of Pharmacy,, Chengdu UniversitySchool of Life Science, Leshan Normal University, Leshan, China, Leshan Normal University01102024251079781311012025Copyright ©; 2024, Bentham Science Publishers2024Bentham Science Publishershttps://journals.eco-vector.com/1389-2037/article/view/645429

: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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