Targeting of DNA gyrase in Streptococcus pneumoniae by sparfloxacin: Selective targeting of gyrase or topoisomerase IV by quinolones
Targeting of DNA gyrase in Streptococcus pneumoniae by sparfloxacin: Selective targeting of gyrase or topoisomerase IV by quinolones
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DOI：
10.1128/aac.41.2.471
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发表时间：
1997-02-01
影响因子：
4.9
通讯作者：
Fisher, LM
中科院分区：
文献类型：
--
作者：
Pan, XS;Fisher, LM
已在逐步选择的耐司帕沙星（一种抗肺炎球菌氟喹诺酮类药物）的肺炎链球菌突变体中鉴定出 gyrA 和 parC 突变。在检查的所有 17 个第一步突变体中都发现了 GyrA 突变（位于相当于大肠杆菌 GyrA 中的耐药热点 Ser-83 的位置），并且先于 DNA 拓扑异构酶 IV ParC 突变（位于 Ser-79 或 Glu-83），而后者仅出现在第二步突变体中。肺炎链球菌中司帕沙星靶向旋转酶，而环丙沙星靶向拓扑异构酶 IV，这表明靶点偏好可以通过喹诺酮结构的变化而改变。
gyrA and parC mutations have been identified in 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.