Quinolones: Mechanism, Lethality and Their Contributions to Antibiotic Resistance.

Quinolones: Mechanism, Lethality and Their Contributions to Antibiotic Resistance.
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DOI:
10.3390/molecules25235662
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发表时间:
2020-12-01
期刊:
Molecules (Basel, Switzerland)
影响因子:
--
通讯作者:
Maxwell A
Maxwell A
中科院分区:
其他
文献类型:
--
作者:
Bush NG;Diez-Santos I;Abbott LR;Maxwell A

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氟喹诺酮类(FQs)可以说是最近最成功的抗生素之一。它们已经在临床上使用了30多年,并成为临床治疗的重要工具。FQs靶向细菌酶DNA促旋酶和DNA拓扑异构酶IV,在那里它们稳定共价酶-DNA复合物,其中DNA在两条链中被切割。这会导致细胞死亡,并成为杀死细菌的一种非常有效的方法。然而,对FQs的耐药性越来越成问题,迫切需要替代化合物。在这里,我们回顾了FQs的作用机制,并讨论了导致细胞死亡的潜在途径。我们还讨论了喹诺酮类药物的耐药性以及喹诺酮类药物治疗如何导致非喹诺酮类抗生素的耐药性。
Fluoroquinolones (FQs) are arguably among the most successful antibiotics of recent times. They have enjoyed over 30 years of clinical usage and become essential tools in the armoury of clinical treatments. FQs target the bacterial enzymes DNA gyrase and DNA topoisomerase IV, where they stabilise a covalent enzyme-DNA complex in which the DNA is cleaved in both strands. This leads to cell death and turns out to be a very effective way of killing bacteria. However, resistance to FQs is increasingly problematic, and alternative compounds are urgently needed. Here, we review the mechanisms of action of FQs and discuss the potential pathways leading to cell death. We also discuss quinolone resistance and how quinolone treatment can lead to resistance to non-quinolone antibiotics.
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