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首页> 外文期刊>Journal of Medicinal Chemistry >Basis for Design and Development of Platinum(IV) Anticancer Complexes
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Basis for Design and Development of Platinum(IV) Anticancer Complexes

机译：铂类（IV）抗癌复合物设计与开发的依据

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Platinum(II) complexes are widely employed in cancer chemotherapy, but their efficacy against the majority of malignancies is limited. The reasons for this failure are a combination of uni- and multicellular resistance, toxicity, and poor whole-body or cellular pharmacokinetic profiles. The discovery, chemistry,and biology of platinum drugs have been extensively reviewed in the literature. Briefly, it is generally accepted that platinum drugs effect their cytotoxic action by entering the cell and binding to DNA. This DNA lesion is recognized by nuclear housekeeping proteins that initiate the apoptotic cascade that leads to cell death, though it is noted that a number of alternative cellular targets have also been proposed.Cellular resistance to cisplatin is largely attributed to up-regulation of DNA repair and damage tolerance pathways, lowered intracellular accumulation, and inactivation by thiol containing reductants such as glutathione and metallothionein. Before arriving at their ultimate target, a large proportion of platinum(II) drugs are lost because of protein binding in the bloodstream and side reactions leading to undesirable side effects.
机译：铂（II）配合物广泛用于癌症化学疗法，但它们对抗大多数恶性肿瘤的功效有限。失败的原因是单细胞和多细胞耐药性，毒性以及不良的全身或细胞药代动力学特征共同作用。铂药物的发现，化学和生物学已在文献中进行了广泛的综述。简而言之，人们普遍接受铂类药物通过进入细胞并与DNA结合而发挥其细胞毒性作用。这种DNA损伤被启动细胞凋亡级联反应并导致细胞死亡的核内务蛋白质所识别，尽管注意到还提出了许多其他的细胞靶标。细胞对顺铂的耐药性主要归因于DNA修复的上调和损伤耐受途径，降低的细胞内蓄积以及含硫醇的还原剂（如谷胱甘肽和金属硫蛋白）的失活。在达到其最终目标之前，由于血液中的蛋白质结合和副反应导致不良副作用，导致大量的铂（II）药物丢失。

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