DNA topoisomerase targets of the fluoroquinolones: A strategy for avoiding bacterial resistance

Xilin Zhao; Chen Xu; John Domagala

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DNA topoisomerase targets of the fluoroquinolones: A strategy for avoiding bacterial resistance

机译：氟喹诺酮类药物的DNA拓扑异构酶靶标：避免细菌耐药性的策略

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Fluoroquinolones are antibacterial agents that attack DNA gyrase and topoisomerase IV on chromo- somal DNA. The existence of two fluoroquinolone targets and stepwise accumulation of resistance suggested that new quin- olones could be found that would require cells to obtain two topoisomerase mutations to display resistance. For wild-type cells to become resistant, the two mutations must be acquired concomitantly. That is expected to occur infrequently. To identify such compounds, fluoroquinolones were tested for the ability to kill a moderately resistant gyrase mutant.

机译：氟喹诺酮类是攻击染色体DNA上的DNA促旋酶和拓扑异构酶IV的抗菌剂。两个氟喹诺酮靶标的存在和耐药性的逐步积累表明，可以发现新的喹诺酮类药物，这些喹诺酮需要细胞获得两个拓扑异构酶突变才能显示出耐药性。为了使野生型细胞具有抗性，必须同时获得两个突变。预计这种情况很少发生。为了鉴定此类化合物，测试了氟喹诺酮类杀死中等抵抗力的促旋酶突变体的能力。

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《Proceedings of the National Academy of Sciences of the United States of America》 |1997年第25期|p.13991-13996|共6页
作者
Xilin Zhao; Chen Xu; John Domagala;
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收录信息美国《科学引文索引》(SCI);美国《生物学医学文摘》(MEDLINE);美国《化学文摘》(CA);
原文格式 PDF
正文语种 eng
中图分类自然科学总论;
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专利

1. Fluoroquinolone resistance in Mycoplasma gallisepticum: DNA gyrase as primary target of enrofloxacin and impact of mutations in topoisomerases on resistance level. [J] . Reinhardt AK, Kempf I, Kobisch M, The Journal of Antimicrobial Chemotherapy . 2002,第4期

机译：鸡败血支原体中的氟喹诺酮耐药性：DNA促旋酶作为恩诺沙星的主要靶标，拓扑异构酶突变对耐药性的影响。
2. Type II topoisomerase mutations in fluoroquinolone-resistant clinical strains of Pseudomonas aeruginosa isolated in 1998 and 1999: role of target enzyme in mechanism of fluoroquinolone resistance. [J] . Akasaka T, Tanaka M, Yamaguchi A, Antimicrobial agents and chemotherapy. . 2001,第8期

机译：1998年和1999年分离的氟喹啉酮型铜绿假单胞菌含氟喹啉酮型临床菌株II型拓扑菌突变：靶酶在氟喹啉耐药机理中的作用。
3. Role of DNA gyrase and topoisomerase IV mutations in fluoroquinolone resistance of Capnocytophaga spp. clinical isolates and laboratory mutants [J] . Ehrmann Elodie, Jolivet-Gougeon Anne, Bonnaure-Mallet Martine, The Journal of Antimicrobial Chemotherapy . 2017,第8期

机译：DNA乙酸酯和拓扑异构酶IV突变在Capnocytophaga SPP氟喹啉酮中的作用。临床分离物和实验室突变体
4. Continuous using of antimicrobial agents less than 6 months or using non-fluoroquinolone antimicrobial agents reduced the occurrence of spontaneous bacterial peritonitis and improved the survival rates in cirrhosis: A meta-analysis [C] . Li-hui Long, Ya-ting Lv, Li Xu, International Conference on Biological Information and Biomedical Engineering . 2018

机译：连续使用少于6个月或使用非氟喹诺酮抗微生物剂的抗菌药物减少了自发性细菌性腹膜炎的发生，并改善了肝硬化的存活率：Meta分析
5. Investigating the fluoroquinolone-topoisomerase interaction by use of novel fluoroquinolone and quinazoline analogs. [D] . Marks, Kevin Randall. 2011

机译：通过使用新型的氟喹诺酮和喹唑啉类似物研究氟喹诺酮-拓扑异构酶的相互作用。
6. DNA topoisomerase targets of the fluoroquinolones: A strategy for avoiding bacterial resistance [O] . Xilin Zhao, Chen Xu, John Domagala, 1997

机译：氟喹诺酮类药物的DNA拓扑异构酶靶标：避免细菌耐药性的策略
7. Quinolone resistance mutations in topoisomerase IV: relationship to the flqA locus and genetic evidence that topoisomerase IV is the primary target and DNA gyrase is the secondary target of fluoroquinolones in Staphylococcus aureus [O] . E Y Ng, M Trucksis, D C Hooper 1996

机译：喹啉酶酶IV中的喹啉抗突变：与拓扑异构酶IV是初级靶标和DNA乙酶的关系，DNA乙酶是金黄色葡萄球菌中氟喹啉酮的二级靶标

DNA topoisomerase targets of the fluoroquinolones: A strategy for avoiding bacterial resistance

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