Antibacterial action of quinolones: from target to network.

Abstract:

:Quinolones are widely used broad-spectrum antibacterials with incomplete elucidated mechanism of action. Here, molecular basis for the antibacterial action of quinolones, from target to network, is fully discussed and updated. Quinolones trap DNA gyrase or topoisomerase IV to form reversible drug-enzyme-DNA cleavage complexes, resulting in bacteriostasis. Cell death arises from chromosome fragmentation in protein synthesis-dependent or -independent pathways according to distinguished quinolone structures. In the former pathway, irreversible oxidative DNA damage caused by reactive oxygen species kills bacteria eventually. Toxin-antitoxin mazEF is triggered as an additional lethal action. Bacteria survive and develop resistance by SOS and other stress responses. Enlarged knowledges of quinolone actions and bacterial response will provide new targets for drug design and approaches to prevent bacterial resistance.

journal_name

Eur J Med Chem

authors

Cheng G,Hao H,Dai M,Liu Z,Yuan Z

doi

10.1016/j.ejmech.2013.01.057

subject

Has Abstract

pub_date

2013-08-01 00:00:00

pages

555-62

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(13)00125-6

journal_volume

66

pub_type

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