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

ABSTRACT: 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.

SUBMITTER: Bush NG

PROVIDER: S-EPMC7730664 | biostudies-literature | 2020 Dec

REPOSITORIES: biostudies-literature

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

Bush Natassja G NG Diez-Santos Isabel I Abbott Lauren R LR Maxwell Anthony A

Molecules (Basel, Switzerland) 20201201 23

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 increasing ...[more]

PMID: 33271787

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