Mechanism of action of cis-dichlorodiammineplatinum(II).
Mechanism of action of cis-dichlorodiammineplatinum(II).
复制标题
顺式二氯二氨铂(II)的作用机制。
DOI：
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发表时间：
1979
期刊：
影响因子：
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通讯作者：
K. Kohn
中科院分区：
文献类型：
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作者：
L. Zwelling;K. Kohn
虽然顺式二氯二胺铂(II)的作用机制尚不明确，但关于其抗肿瘤作用已有很多发现。虽然铂络合物在血浆中是中性的，但它会在细胞内形成带正电的铂物种，很可能与亲核位点相互作用。DNA的嘌呤和嘧啶碱基具有这样的位置，为大多数生物有效的细胞内铂结合提供了场所。虽然有几种类型的结合是可能的，但生物学上重要的损伤最有可能是链间和/或链内交叉连接。这些损伤的形成程度和细胞修复速度可能决定顺式二氯二胺铂(II)对细胞的最终作用。
Although the mechanism of action of cis-dichlorodiammineplatinum(II) is not definitely known, much has been discovered regarding its antitumor effect. Although neutral in plasma, the platinum complex becomes aquated intracellularly to form a positively charged platinum species that is likely to interact with nucleophilic sites. The purine and pyrimidine bases of DNA possess such sites and provide the locale for the majority of the biologically effective intracellular platinum binding. Although several types of binding are possible, the biologically important lesions are most likely interstrand and/or intrastrand cross-links. The extent of formation and the rate of cellular repair of these lesions may determine the ultimate effect of cis-dichlorodiammineplatinum(II) on the cell.