INHIBITION OF TOPOISOMERASE-I BY ANTHRACYCLINE ANTIBIOTICS - EVIDENCE FOR GENERAL INHIBITION OF TOPOISOMERASE-I BY DNA-BINDING AGENTS

被引:26
作者
CROW, RT [1 ]
CROTHERS, DM [1 ]
机构
[1] YALE UNIV,STERLING CHEM LAB,NEW HAVEN,CT 06511
关键词
D O I
10.1021/jm00045a026
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Inhibition of eukaryotic topoisomerase I by daunomycin and structurally modified daunomycin analogues is demonstrated. These studies suggest that binding of the drug to DNA, at low ratios of drug to base pairs of DNA, is sufficient for inhibition that is nonspecific, i.e., inhibition that does not involve the trapping of covalent DNA-topoisomerase I cleavable complexes. Inhibition of numerous DNA-processing enzymes by DNA-binding agents is also implicated.
引用
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页码:3191 / 3194
页数:4
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