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通过限制酶活性抑制评估对映体铂配合物与DNA的不同结合

Different binding to DNA of enantiomeric platinum complexes assessed by inhibition of restriction enzyme activity.

作者信息

Coluccia M, Giordano D, Loseto F, Intini F P, Maresca L, Natile G

机构信息

Istituto di Patologia Generale, Bari, Italy.

出版信息

Anticancer Res. 1989 May-Jun;9(3):795-8.

PMID:2548438
Abstract

The ability of enantiomeric platinum complexes to block the action of selected restriction enzymes has been investigated. The complexes [PtCl2(DAC)], [PtCl2(DAB)] and [PtCl2(DAP)] (DAC = 1,2-diamminocyclohexane; DAB = 2,3-diamminobutane; DAP = 1,2-diamminopropane) exhibit a guanine-cytosine preference in accord with previous results on cis-[PtCl2(NH3)2] (cis-DDP). The extent of inhibition, however, is significantly different for the different isomers; the R,R form is more active than the others at short incubation time, as the time becomes longer, the differences among isomers level off. It also appears that cis-DDP is more active than [PtCl2(DAC)] in blocking the Cfo I enzyme, though it shows a preference for the G-X-G sequences.

摘要

对映体铂配合物阻断所选限制酶作用的能力已得到研究。配合物[PtCl2(DAC)]、[PtCl2(DAB)]和[PtCl2(DAP)](DAC = 1,2 - 二氨基环己烷;DAB = 2,3 - 二氨基丁烷;DAP = 1,2 - 二氨基丙烷)表现出鸟嘌呤 - 胞嘧啶偏好性,这与之前关于顺式[PtCl2(NH3)2](顺铂)的结果一致。然而,不同异构体的抑制程度有显著差异;在短孵育时间时,R,R形式比其他形式更具活性,随着时间延长,异构体之间的差异趋于平稳。似乎顺铂在阻断Cfo I酶方面比[PtCl2(DAC)]更具活性,尽管它对G - X - G序列表现出偏好性。

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