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 Chemjournal_title
European journal of medicinal chemistryauthors
Cheng G,Hao H,Dai M,Liu Z,Yuan Zdoi
10.1016/j.ejmech.2013.01.057subject
Has Abstractpub_date
2013-08-01 00:00:00pages
555-62eissn
0223-5234issn
1768-3254pii
S0223-5234(13)00125-6journal_volume
66pub_type
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