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第二代铂类细胞抑制剂与脱氧核糖核酸的反应

Reaction of platinum cytostatics of the second generation with deoxyribonucleic acid.

作者信息

Kleinwächter V, Rau H

出版信息

Drugs Exp Clin Res. 1986;12(6-7):523-5.

PMID:3743370
Abstract

Adducts of native calf thymus DNA with several platinum compounds with or without antitumour activity were prepared and their chiroptical and renaturation properties investigated. It was found that at high levels of binding cis-dichlorodiammineplatinum(II) and all other substances with antitumour activity induced changes in circular dichroic spectra of DNA which were attributed to formation of "premelted" regions in the double-stranded DNA. On the other hand, the substances with no antitumour effect induced changes corresponding to formation of single-stranded regions in DNA molecules, even at low levels of binding.

摘要

制备了天然小牛胸腺DNA与几种具有或不具有抗肿瘤活性的铂化合物的加合物,并研究了它们的旋光和复性性质。发现,在高结合水平下,顺二氯二氨铂(II)和所有其他具有抗肿瘤活性的物质会诱导DNA圆二色光谱发生变化,这归因于双链DNA中“预熔解”区域的形成。另一方面,即使在低结合水平下,没有抗肿瘤作用的物质也会诱导与DNA分子中单链区域形成相对应的变化。

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