司帕沙星对肺炎链球菌中DNA回旋酶的靶向作用：喹诺酮类药物对回旋酶或拓扑异构酶IV的选择性靶向作用
Targeting of DNA gyrase in Streptococcus pneumoniae by sparfloxacin: selective targeting of gyrase or topoisomerase IV by quinolones.
作者信息
Pan X S, Fisher L M
机构信息
Department of Cellular and Molecular Sciences, St. George's Hospital Medical School, University of London, United Kingdom.
出版信息
Antimicrob Agents Chemother. 1997 Feb;41(2):471-4. doi: 10.1128/AAC.41.2.471.
Abstract
gyrA and parC mutations have been identified inn Streptococcus pneumoniae mutants stepwise selected for resistance to sparfloxacin, an antipneumococcal fluoroquinolone. GyrA mutations (at the position equivalent to resistance hot spot Ser-83 in Escherichia coli GyrA) were found in all 17 first-step mutants examined and preceded DNA topoisomerase IV parC mutations (at Ser-79 or Glu-83), which appeared only in second-step mutants. The targeting of gyrase by sparfloxacin in S. pneumoniae but of topoisomerase IV by ciprofloxacin indicates that target preference can be altered by changes in quinolone structure.
摘要
在逐步选择对抗肺炎球菌氟喹诺酮类药物司帕沙星耐药的肺炎链球菌突变体中，已鉴定出gyrA和parC突变。在所有检测的17个第一步突变体中均发现了GyrA突变（位于与大肠杆菌GyrA中耐药热点Ser-83等效的位置），且该突变先于DNA拓扑异构酶IV的parC突变（位于Ser-79或Glu-83）出现，后者仅出现在第二步突变体中。司帕沙星在肺炎链球菌中靶向gyrase，而环丙沙星靶向拓扑异构酶IV，这表明喹诺酮结构的改变可改变靶点偏好性。
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