Targeting bacterial topoisomerases: how to counter mechanisms of resistance
Date of this Version
6-1-2016
Document Type
Article
Rights
default
Abstract
DNA gyrase and topoisomerase IV are type IIA bacterial topoisomerases that are targeted by highly effective antibiotics. However, resistance via multiple mechanisms arises to limit the efficacies of these drugs. Continued research on type IIA bacterial topoisomerases has provided novel approaches to counter the most common resistance mechanism for utilization of these proven targets in antibacterial therapy. Bacterial topoisomerase I is being explored as an alternative target that is not expected to show cross-resistance. Dual targeting or combination therapy could be strategies for circumventing the development of resistance to topoisomerase-targeting antibiotics. Bacterial topoisomerases are high-value bactericidal targets that could continue to be exploited for antibacterial therapy, if new tactics to counter resistance can be adopted.
DOI
10.4155/fmc-2016-0042
Identifier
27285067
Recommended Citation
Tse-Dinh YC. Targeting bacterial topoisomerases: how to counter mechanisms of resistance. Future Med Chem. 2016 Jun;8(10):1085-100. doi: 10.4155/fmc-2016-0042. Epub 2016 Jun 10. PMID: 27285067.
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