• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利：CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法，用中文像聊天一样搜索，搜遍4000万医学文献。AI智能推荐，让科研检索更轻松。

立即免费搜索

文件翻译

保留排版，准确专业，支持PDF/Word/PPT等文件格式，支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述，25分钟生成高质量综述，智能提取关键信息，辅助科研写作。

立即免费体验

格帕沙星，环丙沙星的二甲基衍生物，在肺炎链球菌中主要通过拓扑异构酶起作用：C-5基团在靶点特异性中的作用。

Grepafloxacin, a dimethyl derivative of ciprofloxacin, acts preferentially through gyrase in Streptococcus pneumoniae: role of the C-5 group in target specificity.

作者信息

Morris Julia E, Pan Xiao-Su, Fisher L Mark

机构信息

Molecular Genetics Group, Department of Biochemistry and Immunology, St. George's Hospital Medical School, University of London, London SW17 0RE, United Kingdom.

出版信息

Antimicrob Agents Chemother. 2002 Feb;46(2):582-5. doi: 10.1128/AAC.46.2.582-585.2002.

DOI:10.1128/AAC.46.2.582-585.2002
PMID:11796384
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC127062/
Abstract

Grepafloxacin, a 5-methyl-7-piperazinyl-3"-methyl analogue of ciprofloxacin, was used to obtain stepwise-selected mutants of Streptococcus pneumoniae 7785. Analysis of the quinolone resistance-determining regions of the gyrA, gyrB, parC, and parE genes in these mutants revealed that gyrA mutations preceded those in parC. Given that ciprofloxacin (5-H,7-piperazinyl) and AM-1121 (5-H,7-piperazinyl-3"-methyl) both act through topoisomerase IV, we conclude that the 5-methyl group of grepafloxacin favors gyrase in S. pneumoniae.

摘要

格帕沙星是环丙沙星的5-甲基-7-哌嗪基-3''-甲基类似物，用于获得肺炎链球菌7785的逐步选择突变体。对这些突变体中gyrA、gyrB、parC和parE基因的喹诺酮耐药决定区进行分析，结果显示gyrA突变先于parC突变。鉴于环丙沙星（5-H，7-哌嗪基）和AM-1121（5-H，7-哌嗪基-3''-甲基）均通过拓扑异构酶IV发挥作用，我们得出结论，格帕沙星的5-甲基基团有利于肺炎链球菌中的gyrase。

相似文献

1
Grepafloxacin, a dimethyl derivative of ciprofloxacin, acts preferentially through gyrase in Streptococcus pneumoniae: role of the C-5 group in target specificity.格帕沙星，环丙沙星的二甲基衍生物，在肺炎链球菌中主要通过拓扑异构酶起作用：C-5基团在靶点特异性中的作用。
Antimicrob Agents Chemother. 2002 Feb;46(2):582-5. doi: 10.1128/AAC.46.2.582-585.2002.
2
DNA gyrase and topoisomerase IV are dual targets of clinafloxacin action in Streptococcus pneumoniae.DNA 回旋酶和拓扑异构酶IV是环丙沙星作用于肺炎链球菌的双重靶点。
Antimicrob Agents Chemother. 1998 Nov;42(11):2810-6. doi: 10.1128/AAC.42.11.2810.
3
Ciprofloxacin dimers target gyrase in Streptococcus pneumoniae.环丙沙星二聚体靶向肺炎链球菌中的回旋酶。
Antimicrob Agents Chemother. 2004 Jun;48(6):2108-15. doi: 10.1128/AAC.48.6.2108-2115.2004.
4
Involvement of topoisomerase IV and DNA gyrase as ciprofloxacin targets in Streptococcus pneumoniae.拓扑异构酶IV和DNA促旋酶作为环丙沙星在肺炎链球菌中的作用靶点。
Antimicrob Agents Chemother. 1996 Oct;40(10):2321-6. doi: 10.1128/AAC.40.10.2321.
5
Quinolone resistance mutations in Streptococcus pneumoniae GyrA and ParC proteins: mechanistic insights into quinolone action from enzymatic analysis, intracellular levels, and phenotypes of wild-type and mutant proteins.肺炎链球菌GyrA和ParC蛋白中的喹诺酮耐药性突变：基于酶分析、细胞内水平以及野生型和突变型蛋白表型对喹诺酮作用机制的深入了解
Antimicrob Agents Chemother. 2001 Nov;45(11):3140-7. doi: 10.1128/AAC.45.11.3140-3147.2001.
6
Relationship between mutations in parC and gyrA of clinical isolates of Streptococcus pneumoniae and resistance to ciprofloxacin and grepafloxacin.肺炎链球菌临床分离株parC和gyrA基因突变与对环丙沙星和格帕沙星耐药性的关系。
J Med Microbiol. 1999 Dec;48(12):1103-1106. doi: 10.1099/00222615-48-12-1103.
7
Engineering the specificity of antibacterial fluoroquinolones: benzenesulfonamide modifications at C-7 of ciprofloxacin change its primary target in Streptococcus pneumoniae from topoisomerase IV to gyrase.设计抗菌氟喹诺酮类药物的特异性：环丙沙星C-7位的苯磺酰胺修饰将其在肺炎链球菌中的主要靶点从拓扑异构酶IV转变为回旋酶。
Antimicrob Agents Chemother. 2000 Feb;44(2):320-5. doi: 10.1128/AAC.44.2.320-325.2000.
8
Cloning and characterization of the parC and parE genes of Streptococcus pneumoniae encoding DNA topoisomerase IV: role in fluoroquinolone resistance.肺炎链球菌编码DNA拓扑异构酶IV的parC和parE基因的克隆与特性分析：在氟喹诺酮耐药性中的作用
J Bacteriol. 1996 Jul;178(14):4060-9. doi: 10.1128/jb.178.14.4060-4069.1996.
9
Potent antipneumococcal activity of gemifloxacin is associated with dual targeting of gyrase and topoisomerase IV, an in vivo target preference for gyrase, and enhanced stabilization of cleavable complexes in vitro.吉米沙星强大的抗肺炎球菌活性与对回旋酶和拓扑异构酶IV的双重靶向作用、在体内对回旋酶的靶点偏好以及在体外增强可裂解复合物的稳定性有关。
Antimicrob Agents Chemother. 2000 Nov;44(11):3112-7. doi: 10.1128/AAC.44.11.3112-3117.2000.
10
Cleavable-complex formation by wild-type and quinolone-resistant Streptococcus pneumoniae type II topoisomerases mediated by gemifloxacin and other fluoroquinolones.吉米沙星和其他氟喹诺酮介导的野生型和耐喹诺酮肺炎链球菌II型拓扑异构酶形成可裂解复合物
Antimicrob Agents Chemother. 2002 Feb;46(2):413-9. doi: 10.1128/AAC.46.2.413-419.2002.

引用本文的文献

1
Contribution of the ATP binding site of ParE to susceptibility to novobiocin and quinolones in Streptococcus pneumoniae.肺炎链球菌中ParE的ATP结合位点对新生霉素和喹诺酮敏感性的贡献。
J Bacteriol. 2005 Feb;187(4):1536-40. doi: 10.1128/JB.187.4.1536-1540.2005.
2
Mycobacterium tuberculosis DNA gyrase: interaction with quinolones and correlation with antimycobacterial drug activity.结核分枝杆菌DNA回旋酶：与喹诺酮类药物的相互作用及其与抗分枝杆菌药物活性的相关性。
Antimicrob Agents Chemother. 2004 Apr;48(4):1281-8. doi: 10.1128/AAC.48.4.1281-1288.2004.
3
Topoisomerase targeting with and resistance to gemifloxacin in Staphylococcus aureus.金黄色葡萄球菌中吉米沙星对拓扑异构酶的靶向作用及耐药性
Antimicrob Agents Chemother. 2003 Jan;47(1):274-82. doi: 10.1128/AAC.47.1.274-282.2003.

本文引用的文献

1
Quinolone resistance mutations in Streptococcus pneumoniae GyrA and ParC proteins: mechanistic insights into quinolone action from enzymatic analysis, intracellular levels, and phenotypes of wild-type and mutant proteins.肺炎链球菌GyrA和ParC蛋白中的喹诺酮耐药性突变：基于酶分析、细胞内水平以及野生型和突变型蛋白表型对喹诺酮作用机制的深入了解
Antimicrob Agents Chemother. 2001 Nov;45(11):3140-7. doi: 10.1128/AAC.45.11.3140-3147.2001.
2
Contributions of the 8-methoxy group of gatifloxacin to resistance selectivity, target preference, and antibacterial activity against Streptococcus pneumoniae.加替沙星的8-甲氧基对肺炎链球菌耐药选择性、靶点偏好性及抗菌活性的作用
Antimicrob Agents Chemother. 2001 Jun;45(6):1649-53. doi: 10.1128/AAC.45.6.1649-1653.2001.
3
Fluoroquinolones inhibit preferentially Streptococcus pneumoniae DNA topoisomerase IV than DNA gyrase native proteins.氟喹诺酮类药物对肺炎链球菌DNA拓扑异构酶IV的抑制作用比对DNA促旋酶天然蛋白的抑制作用更强。
Microb Drug Resist. 2000 Winter;6(4):259-67. doi: 10.1089/mdr.2000.6.259.
4
Potent antipneumococcal activity of gemifloxacin is associated with dual targeting of gyrase and topoisomerase IV, an in vivo target preference for gyrase, and enhanced stabilization of cleavable complexes in vitro.吉米沙星强大的抗肺炎球菌活性与对回旋酶和拓扑异构酶IV的双重靶向作用、在体内对回旋酶的靶点偏好以及在体外增强可裂解复合物的稳定性有关。
Antimicrob Agents Chemother. 2000 Nov;44(11):3112-7. doi: 10.1128/AAC.44.11.3112-3117.2000.
5
Purification of pneumococcal type II topoisomerases and inhibition by gemifloxacin and other quinolones.II型肺炎链球菌拓扑异构酶的纯化及吉米沙星和其他喹诺酮类药物对其的抑制作用
J Antimicrob Chemother. 2000 Apr;45 Suppl 1:101-6. doi: 10.1093/jac/45.suppl_3.101.
6
Intracellular targets of moxifloxacin: a comparison with other fluoroquinolones.莫西沙星的细胞内靶点：与其他氟喹诺酮类药物的比较。
J Antimicrob Chemother. 2000 May;45(5):583-90. doi: 10.1093/jac/45.5.583.
7
Engineering the specificity of antibacterial fluoroquinolones: benzenesulfonamide modifications at C-7 of ciprofloxacin change its primary target in Streptococcus pneumoniae from topoisomerase IV to gyrase.设计抗菌氟喹诺酮类药物的特异性：环丙沙星C-7位的苯磺酰胺修饰将其在肺炎链球菌中的主要靶点从拓扑异构酶IV转变为回旋酶。
Antimicrob Agents Chemother. 2000 Feb;44(2):320-5. doi: 10.1128/AAC.44.2.320-325.2000.
8
Relationship between mutations in parC and gyrA of clinical isolates of Streptococcus pneumoniae and resistance to ciprofloxacin and grepafloxacin.肺炎链球菌临床分离株parC和gyrA基因突变与对环丙沙星和格帕沙星耐药性的关系。
J Med Microbiol. 1999 Dec;48(12):1103-1106. doi: 10.1099/00222615-48-12-1103.
9
Dual inhibitory activity of sitafloxacin (DU-6859a) against DNA gyrase and topoisomerase IV of Streptococcus pneumoniae.司帕沙星（DU-6859a）对肺炎链球菌DNA旋转酶和拓扑异构酶IV的双重抑制活性。
J Antimicrob Chemother. 1999 Oct;44(4):533-6. doi: 10.1093/jac/44.4.533.
10
Activities of fluoroquinolones against Streptococcus pneumoniae type II topoisomerases purified as recombinant proteins.氟喹诺酮类药物对作为重组蛋白纯化的II型肺炎链球菌拓扑异构酶的活性。
Antimicrob Agents Chemother. 1999 Nov;43(11):2579-85. doi: 10.1128/AAC.43.11.2579.