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Antibiotics 2017, 6(4), 26; doi:10.3390/antibiotics6040026

Ubiquitous Nature of Fluoroquinolones: The Oscillation between Antibacterial and Anticancer Activities

Department of Chemistry, University of Manitoba, Winnipeg, MB R3T 2N2, Canada
Department of Medical Microbiology and Infectious Diseases, University of Manitoba, Winnipeg, MB R3T 1R9, Canada
Author to whom correspondence should be addressed.
Received: 30 September 2017 / Revised: 26 October 2017 / Accepted: 3 November 2017 / Published: 7 November 2017
(This article belongs to the Special Issue Top 35 of Antibiotics Travel Awards 2017)
View Full-Text   |   Download PDF [1554 KB, uploaded 7 November 2017]   |  


Fluoroquinolones are synthetic antibacterial agents that stabilize the ternary complex of prokaryotic topoisomerase II enzymes (gyrase and Topo IV), leading to extensive DNA fragmentation and bacteria death. Despite the similar structural folds within the critical regions of prokaryotic and eukaryotic topoisomerases, clinically relevant fluoroquinolones display a remarkable selectivity for prokaryotic topoisomerase II, with excellent safety records in humans. Typical agents that target human topoisomerases (such as etoposide, doxorubicin and mitoxantrone) are associated with significant toxicities and secondary malignancies, whereas clinically relevant fluoroquinolones are not known to exhibit such propensities. Although many fluoroquinolones have been shown to display topoisomerase-independent antiproliferative effects against various human cancer cells, those that are significantly active against eukaryotic topoisomerase show the same DNA damaging properties as other topoisomerase poisons. Empirical models also show that fluoroquinolones mediate some unique immunomodulatory activities of suppressing pro-inflammatory cytokines and super-inducing interleukin-2. This article reviews the extended roles of fluoroquinolones and their prospects as lead for the unmet needs of “small and safe” multimodal-targeting drug scaffolds. View Full-Text
Keywords: antibacterial; antiproliferative; antitumor; fluoroquinolone; gyrase; immunomodulation; topoisomerase antibacterial; antiproliferative; antitumor; fluoroquinolone; gyrase; immunomodulation; topoisomerase

This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Idowu, T.; Schweizer, F. Ubiquitous Nature of Fluoroquinolones: The Oscillation between Antibacterial and Anticancer Activities. Antibiotics 2017, 6, 26.

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