The interaction of drugs with DNA gyrase: A model for the molecular basis of quinolone action

被引：62

作者：

Heddle, JG ^{[1
]}

Barnard, FM ^{[1
]}

Wentzell, LM ^{[1
]}

Maxwell, A ^{[1
]}

机构：

[1] Univ Leicester, Dept Biochem, Leicester LE1 7RH, Leics, England

来源：

NUCLEOSIDES NUCLEOTIDES & NUCLEIC ACIDS | 2000年 / 19卷 / 08期

关键词：

D O I：

10.1080/15257770008033048

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

DNA gyrase supercoils DNA in bacteria. The fact that it is essential in all bacteria and absent from eukaryotes makes it an ideal drug target. We discuss the action of coumarin and quinolone drugs on gyrase. In the case of coumarins, the drugs are known to be competitive inhibitors of the gyrase ATPase reaction. From a combination of structural and biochemical studies, the molecular details of the gyrase-coumarin complex are well established. In the case of quinolones, the drugs are thought to act by stabilising a cleavage complex between gyrase and DNA that arrests polymerases in vivo. The exact nature of the gyrase-quinolone-DNA complex is not known; we propose a model for this complex based on structural and biochemical data.

引用

页码：1249 / 1264

页数：18

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