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一种抗肿瘤铂络合物与DNA的相互作用。

The interaction of an anti-tumour platinum complex with DNA.

作者信息

Roos I A

出版信息

Chem Biol Interact. 1977 Jan;16(1):39-55. doi: 10.1016/0009-2797(77)90152-1.

Abstract

The interaction of the anti-tumour active cis platinum (II) complexes with DNA has been investigated using dichloro(ethylenediamine)platinum(II) and E. coli DNA. Equilibrium dialysis studies indicate that Pt(en)Cl2 binds reversibly to DNA to a saturation value of 0.57 Pt: P, which is consistent with the platinum being bound both monofunctionally and bifunctionally. Pt(en)Cl2 inhibits the intercalation of 9-aminoacridine (9AA) by cross-linking the bases of the double helix, but at no stage does all the bound platinum cross-link. It is suggested that this inhibition of intercalation is due to intrastrand cross-linking.

摘要

使用二氯(乙二胺)铂(II)和大肠杆菌DNA研究了抗肿瘤活性顺铂(II)配合物与DNA的相互作用。平衡透析研究表明,Pt(en)Cl2与DNA可逆结合,饱和值为0.57 Pt:P,这与铂以单功能和双功能方式结合一致。Pt(en)Cl2通过交联双螺旋的碱基来抑制9-氨基吖啶(9AA)的嵌入,但在任何阶段,并非所有结合的铂都会发生交联。有人认为这种嵌入抑制是由于链内交联。

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