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Photoactivatable Platinum-Based Anticancer Drugs: Mode of Photoactivation and Mechanism of Action

机译:基于光活性铂的抗癌药物:光激活模式和行动机制

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摘要

Platinum-based anticancer drugs are a class of widely used agents in clinical cancer treatment. However, their efficacy was greatly limited by their severe side effects and the arising drug resistance. The selective activation of inert platinum-based drugs in the tumor site by light irradiation is able to reduce side effects, and the novel mechanism of action of photoactivatable platinum drugs might also conquer the resistance. In this review, the recent advances in the design of photoactivatable platinum-based drugs were summarized. The complexes are classified according to their mode of action, including photoreduction, photo-uncaging, and photodissociation. The rationale of drug design, dark stability, photoactivation process, cytotoxicity, and mechanism of action of typical photoactivatable platinum drugs were reviewed. Finally, the challenges and opportunities for designing more potent photoactivatable platinum drugs were discussed.
机译:基于铂族的抗癌药物是临床癌症治疗中的一类广泛使用的药剂。然而,它们的功效受到严重的副作用和引起的耐药性极大的限制。通过光辐射在肿瘤部位中的惰性铂类药物的选择性活化能够减少副作用,并且光活化铂药物的新作用机制也可能征服抗性。在本综述中,总结了可光激活铂类药物设计的最新进展。复合物根据其作用方式进行分类,包括光电,光未展示和光学探测。综述了药物设计,暗稳定性,光活化过程,细胞毒性和作用机制的基本原理进行了综述。最后,讨论了设计更多有效的光活化铂药的挑战和机会。

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