首页> 美国卫生研究院文献>Antimicrobial Agents and Chemotherapy >Targeting of DNA gyrase in Streptococcus pneumoniae by sparfloxacin: selective targeting of gyrase or topoisomerase IV by quinolones.
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Targeting of DNA gyrase in Streptococcus pneumoniae by sparfloxacin: selective targeting of gyrase or topoisomerase IV by quinolones.

机译:司帕沙星靶向肺炎链球菌中的DNA促旋酶:喹诺酮类药物选择性靶向促旋酶或拓扑异构酶IV。

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摘要

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.
机译:在肺炎链球菌突变体中已鉴定出gyrA和parC突变,这些突变体被逐步选择为对抗肺炎球菌氟喹诺酮司帕沙星具有抗性。 GyrA突变(在大肠杆菌GyrA中与抗性热点Ser-83相当的位置)在所有检查的17个第一步突变体中均发现,且先于DNA拓扑异构酶IV parC突变(在Ser-79或Glu-83中),在第二步突变体中。肺炎链球菌中司帕沙星对陀螺酶的靶向作用,环丙沙星对拓扑异构酶IV的靶向作用表明,靶点的喜好可以通过喹诺酮结构的改变而改变。

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