肺炎链球菌中氟喹诺酮类药物的主要作用靶点。
Primary targets of fluoroquinolones in Streptococcus pneumoniae.
作者信息
Fukuda H, Hiramatsu K
机构信息
Central Research Laboratories, Kyorin Pharmaceutical Co., Ltd., Tochigi, Japan.
出版信息
Antimicrob Agents Chemother. 1999 Feb;43(2):410-2. doi: 10.1128/AAC.43.2.410.
Abstract
Mutants of wild-type Streptococcus pneumoniae IID553 with mutations in parC were obtained by selection with trovafloxacin, levofloxacin, norfloxacin, and ciprofloxacin. All of the parC mutants were cross-resistant to the selecting agents but were not resistant to gatifloxacin and sparfloxacin. On the other hand, gyrA mutants were isolated by selection with gatifloxacin and sparfloxacin. The gyrA mutants were cross-resistant to gatifloxacin and sparfloxacin but were not resistant to the other fluoroquinolones tested. These results suggest that in wild-type S. pneumoniae the primary target of trovafloxacin, levofloxacin, norfloxacin, and ciprofloxacin is topoisomerase IV, whereas the primary target of gatifloxacin and sparfloxacin is DNA gyrase.
摘要
通过使用曲伐沙星、左氧氟沙星、诺氟沙星和环丙沙星进行筛选，获得了野生型肺炎链球菌IID553中parC发生突变的突变体。所有parC突变体对筛选药物均具有交叉耐药性，但对加替沙星和司帕沙星不耐药。另一方面，通过使用加替沙星和司帕沙星进行筛选分离出了gyrA突变体。gyrA突变体对加替沙星和司帕沙星具有交叉耐药性，但对所测试的其他氟喹诺酮类药物不耐药。这些结果表明，在野生型肺炎链球菌中，曲伐沙星、左氧氟沙星、诺氟沙星和环丙沙星的主要靶点是拓扑异构酶IV，而加替沙星和司帕沙星的主要靶点是DNA旋转酶。
相似文献
1
Primary targets of fluoroquinolones in Streptococcus pneumoniae.肺炎链球菌中氟喹诺酮类药物的主要作用靶点。
Antimicrob Agents Chemother. 1999 Feb;43(2):410-2. doi: 10.1128/AAC.43.2.410.
2
Contribution of topoisomerase IV and DNA gyrase mutations in Streptococcus pneumoniae to resistance to novel fluoroquinolones.肺炎链球菌中拓扑异构酶IV和DNA促旋酶突变对新型氟喹诺酮类药物耐药性的影响
Antimicrob Agents Chemother. 1999 Aug;43(8):2000-4. doi: 10.1128/AAC.43.8.2000.
3
Single- and multi-step resistance selection study of gemifloxacin compared with trovafloxacin, ciprofloxacin, gatifloxacin and moxifloxacin in Streptococcus pneumoniae.肺炎链球菌中吉米沙星与曲伐沙星、环丙沙星、加替沙星和莫西沙星的单步及多步耐药性选择研究
J Antimicrob Chemother. 2001 Sep;48(3):365-74. doi: 10.1093/jac/48.3.365.
4
Mutant prevention concentrations for single-step fluoroquinolone-resistant mutants of wild-type, efflux-positive, or ParC or GyrA mutation-containing Streptococcus pneumoniae isolates.野生型、外排阳性或含有ParC或GyrA突变的肺炎链球菌分离株的单步氟喹诺酮耐药突变体的突变预防浓度。
Antimicrob Agents Chemother. 2004 Oct;48(10):3954-8. doi: 10.1128/AAC.48.10.3954-3958.2004.
5
Targeting of DNA gyrase in Streptococcus pneumoniae by sparfloxacin: selective targeting of gyrase or topoisomerase IV by quinolones.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
Antimicrob Agents Chemother. 1997 Feb;41(2):471-4. doi: 10.1128/AAC.41.2.471.
6
Activity of the new fluoroquinolone trovafloxacin (CP-99,219) against DNA gyrase and topoisomerase IV mutants of Streptococcus pneumoniae selected in vitro.新型氟喹诺酮曲伐沙星（CP-99,219）对体外筛选的肺炎链球菌DNA旋转酶和拓扑异构酶IV突变体的活性。
Antimicrob Agents Chemother. 1996 Dec;40(12):2691-7. doi: 10.1128/AAC.40.12.2691.
7
ParC and GyrA may be interchangeable initial targets of some fluoroquinolones in Streptococcus pneumoniae.在肺炎链球菌中，ParC和GyrA可能是某些氟喹诺酮类药物的可互换初始靶点。
Antimicrob Agents Chemother. 1999 Feb;43(2):302-6. doi: 10.1128/AAC.43.2.302.
8
Activities of newer fluoroquinolones against Streptococcus pneumoniae clinical isolates including those with mutations in the gyrA, parC, and parE loci.新型氟喹诺酮类药物对肺炎链球菌临床分离株的活性，包括那些gyrA、parC和parE基因座发生突变的分离株。
Antimicrob Agents Chemother. 1999 Feb;43(2):329-34. doi: 10.1128/AAC.43.2.329.
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
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.
引用本文的文献
1
The mutational landscape of quinolone resistance in Escherichia coli.喹诺酮类耐药大肠杆菌的突变特征。
PLoS One. 2019 Nov 5;14(11):e0224650. doi: 10.1371/journal.pone.0224650. eCollection 2019.
2
Synthetic studies on the reverse antibiotic natural products, the nybomycins.对反向抗生素天然产物尼博霉素的合成研究。
Medchemcomm. 2019 May 24;10(8):1438-1444. doi: 10.1039/c9md00207c. eCollection 2019 Aug 1.
3
In Vitro Resistance Development to Nemonoxacin in Streptococcus pneumoniae: A Unique Profile for a Novel Nonfluorinated Quinolone.肺炎链球菌对奈诺沙星的体外耐药性演变：一种新型非氟喹诺酮类药物的独特特征
Microb Drug Resist. 2016 Oct;22(7):578-584. doi: 10.1089/mdr.2016.0021. Epub 2016 Jun 7.
4
In Vitro and In Vivo Characterization of the Novel Oxabicyclooctane-Linked Bacterial Topoisomerase Inhibitor AM-8722, a Selective, Potent Inhibitor of Bacterial DNA Gyrase.新型氧杂双环辛烷连接的细菌拓扑异构酶抑制剂AM-8722的体外和体内特性，一种细菌DNA促旋酶的选择性强效抑制剂。
Antimicrob Agents Chemother. 2016 Jul 22;60(8):4830-9. doi: 10.1128/AAC.00619-16. Print 2016 Aug.
5
Trends in antibiotic resistance in bacterial keratitis isolates from South India.印度南部细菌性角膜炎分离株的抗生素耐药性趋势
Br J Ophthalmol. 2017 Feb;101(2):108-113. doi: 10.1136/bjophthalmol-2016-308487. Epub 2016 Apr 29.
6
Development and validation of stability-indicating high performance liquid chromatography method to analyze gatifloxacin in bulk drug and pharmaceutical preparations.建立和验证高效液相色谱法测定原料药及制剂中加替沙星的含量及其有关物质。
Saudi Pharm J. 2015 Jan;23(1):85-94. doi: 10.1016/j.jsps.2014.06.005. Epub 2014 Jun 28.
7
Genomic characterization of ciprofloxacin resistance in a laboratory-derived mutant and a clinical isolate of Streptococcus pneumoniae.肺炎链球菌实验室衍生突变株和临床分离株中环丙沙星耐药的基因组特征。
Antimicrob Agents Chemother. 2013 Oct;57(10):4911-9. doi: 10.1128/AAC.00418-13. Epub 2013 Jul 22.
8
The new fluoroquinolones: A critical review.新型氟喹诺酮类药物：批判性综述。
Can J Infect Dis. 1999 May;10(3):207-38. doi: 10.1155/1999/378394.
9
Real-time PCR and high-resolution melt analysis for rapid detection of Mycobacterium leprae drug resistance mutations and strain types.实时聚合酶链反应和高分辨率熔解曲线分析快速检测麻风分枝杆菌耐药突变和菌株类型。
J Clin Microbiol. 2012 Mar;50(3):742-53. doi: 10.1128/JCM.05183-11. Epub 2011 Dec 14.
10
Transmission of dapsone-resistant leprosy detected by molecular epidemiological approaches.分子流行病学方法检测到的耐氨苯砜麻风病传播。
Antimicrob Agents Chemother. 2011 Nov;55(11):5384-7. doi: 10.1128/AAC.05236-11. Epub 2011 Aug 22.
本文引用的文献
1
Antibacterial activity of gatifloxacin (AM-1155, CG5501, BMS-206584), a newly developed fluoroquinolone, against sequentially acquired quinolone-resistant mutants and the norA transformant of Staphylococcus aureus.新型氟喹诺酮类药物加替沙星（AM - 1155、CG5501、BMS - 206584）对金黄色葡萄球菌序贯获得性喹诺酮耐药突变株及norA转化株的抗菌活性。
Antimicrob Agents Chemother. 1998 Aug;42(8):1917-22. doi: 10.1128/AAC.42.8.1917.
2
Molecular characterization of the gene encoding the DNA gyrase A subunit of Streptococcus pneumoniae.肺炎链球菌DNA旋转酶A亚基编码基因的分子特征
J Bacteriol. 1998 Jun;180(11):2854-61. doi: 10.1128/JB.180.11.2854-2861.1998.
3
DNA topoisomerase targets of the fluoroquinolones: a strategy for avoiding bacterial resistance.氟喹诺酮类药物的DNA拓扑异构酶靶点：一种避免细菌耐药性的策略。
Proc Natl Acad Sci U S A. 1997 Dec 9;94(25):13991-6. doi: 10.1073/pnas.94.25.13991.
4
Non-gyrA-mediated ciprofloxacin resistance in laboratory mutants of Streptococcus pneumoniae.肺炎链球菌实验室突变株中不依赖gyrA的环丙沙星耐药性
J Antimicrob Chemother. 1997 May;39(5):609-15. doi: 10.1093/jac/39.5.609.
5
Apparent involvement of a multidrug transporter in the fluoroquinolone resistance of Streptococcus pneumoniae.多药转运蛋白明显参与肺炎链球菌对氟喹诺酮类药物的耐药性。
Antimicrob Agents Chemother. 1997 Jun;41(6):1396-8. doi: 10.1128/AAC.41.6.1396.
6
Characterization of a mutation in the parE gene that confers fluoroquinolone resistance in Streptococcus pneumoniae.肺炎链球菌中赋予氟喹诺酮耐药性的parE基因突变特征分析。
Antimicrob Agents Chemother. 1997 May;41(5):1166-7. doi: 10.1128/AAC.41.5.1166.
7
Differential behaviors of Staphylococcus aureus and Escherichia coli type II DNA topoisomerases.金黄色葡萄球菌和大肠杆菌II型DNA拓扑异构酶的差异行为
Antimicrob Agents Chemother. 1996 Dec;40(12):2714-20. doi: 10.1128/AAC.40.12.2714.
8
Activity of the new fluoroquinolone trovafloxacin (CP-99,219) against DNA gyrase and topoisomerase IV mutants of Streptococcus pneumoniae selected in vitro.新型氟喹诺酮曲伐沙星（CP-99,219）对体外筛选的肺炎链球菌DNA旋转酶和拓扑异构酶IV突变体的活性。
Antimicrob Agents Chemother. 1996 Dec;40(12):2691-7. doi: 10.1128/AAC.40.12.2691.
9
Targeting of DNA gyrase in Streptococcus pneumoniae by sparfloxacin: selective targeting of gyrase or topoisomerase IV by quinolones.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
Antimicrob Agents Chemother. 1997 Feb;41(2):471-4. doi: 10.1128/AAC.41.2.471.
10
Contribution of mutations in gyrA and parC genes to fluoroquinolone resistance of mutants of Streptococcus pneumoniae obtained in vivo and in vitro.gyrA和parC基因突变对体内外获得的肺炎链球菌突变体氟喹诺酮耐药性的影响。
Antimicrob Agents Chemother. 1996 Nov;40(11):2505-10. doi: 10.1128/AAC.40.11.2505.
Zotero 插件