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安吖啶-4-羧酰胺与DNA中富含鸟嘌呤-胞嘧啶序列相互作用时选择性的分子起源

Molecular origins of selectivity in the interaction of amsacrine-4-carboxamide with GC-rich sequences in DNA.

作者信息

Bailly C, Denny W A, Waring M J

机构信息

Institut de Recherches sur le Cancer, INSERM Unité 124, Lille, France.

出版信息

Anticancer Drug Des. 1996 Dec;11(8):611-24.

PMID:9022749
Abstract

To determine the molecular origins of the preferential binding of an antitumour amsacrine-4-carboxamide derivative to GC-rich sequences in DNA, we have used the polymerase chain reaction to synthesize a series of oligodeoxynucleotides in which the position of the purine 2-amino group is varied and then investigated the binding of the drug to normal and modified DNA molecules by means of DNase I footprinting. The results indicate that the 2-amino group of guanine represents an important but not unique element which directs selective binding of amsacrine-4-carboxamides to GC-rich sequences.

摘要

为了确定一种抗肿瘤安吖啶 - 4 - 羧酰胺衍生物与DNA中富含GC序列优先结合的分子起源,我们利用聚合酶链反应合成了一系列嘌呤2 - 氨基位置不同的寡脱氧核苷酸,然后通过DNase I足迹法研究了该药物与正常及修饰DNA分子的结合情况。结果表明,鸟嘌呤的2 - 氨基是指导安吖啶 - 4 - 羧酰胺选择性结合富含GC序列的重要但非唯一的元素。

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