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顺铂耐药肿瘤的挑战性治疗:现状与未来展望。

The Challenging Treatment of Cisplatin-Resistant Tumors: State of the Art and Future Perspectives.

机构信息

Department of Pharmaceutical Sciences, University of Milan, Via Venezian 21, 20133 Milano, Italy.

出版信息

Molecules. 2023 Apr 12;28(8):3407. doi: 10.3390/molecules28083407.

Abstract

One of the main problems in chemotherapy using platinum drugs as anticancer agents is the resistance phenomenon. Synthesizing and evaluating valid alternative compounds is challenging. This review focuses on the last two years of progress in the studies of platinum (II)- and platinum (IV)-based anticancer complexes. In particular, the research studies reported herein focus on the capability of some platinum-based anticancer agents to bypass resistance to chemotherapy, which is typical of well-known drugs such as cisplatin. Regarding platinum (II) complexes, this review deals with complexes in trans conformation; complexes containing bioactive ligands, as well as those that are differently charged, all experience a different reaction mechanism compared with cisplatin. Regarding platinum (IV) compounds, the focus was on complexes with biologically active ancillary ligands that exert a synergistic effect with platinum (II)-active complexes upon reduction, or those for which controllable activation can be realized thanks to intracellular stimuli.

摘要

在使用铂类药物作为抗癌剂进行化疗时,主要问题之一是耐药现象。合成和评估有效的替代化合物具有挑战性。本综述重点介绍了过去两年中在铂(II)和铂(IV)基抗癌配合物研究方面的进展。特别是,本文所述的研究重点关注了一些铂类抗癌药物克服对顺铂等知名药物的化疗耐药性的能力。关于铂(II)配合物,本综述涉及反式构象的配合物;含有生物活性配体的配合物以及带不同电荷的配合物,与顺铂相比,它们的反应机制都有所不同。关于铂(IV)化合物,重点是具有生物活性辅助配体的配合物,这些配合物在还原时与铂(II)活性配合物具有协同作用,或者由于细胞内刺激可以实现可控激活。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3706/10144581/8367587f5f91/molecules-28-03407-g001.jpg

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