DNA topoisomerases as targets for antibacterial agents

Research output: Chapter in Book/Report/Conference proceedingChapter

Abstract

DNA topoisomerases are proven therapeutic targets of antibacterial agents. Quinolones, especially fluoroquinolones, are the most successful topoisomerase-targeting antibacterial drugs. These drugs target type IIA topoisomerases in bacteria. Recent structural and biochemical studies on fluoroquinolones have provided the molecular basis for both their mechanism of action, as well as the molecular basis of bacterial resistance. Due to the development of drug resistance, including fluoroquinolone resistance, among bacterial pathogens, there is an urgent need to discover novel antibacterial agents. Recent advances in topoisomerase inhibitors may lead to the development of novel antibacterial drugs that are effective against fluoroquinolone-resistant pathogens. They include type IIA topoisomerase inhibitors that either interact with the GyrB/ParE subunit or form nick-containing ternary complexes. In addition, several topoisomerase I inhibitors have recently been identified. Thus, DNA topoisomerases remain important targets of antibacterial agents.

LanguageEnglish (US)
Title of host publicationMethods in Molecular Biology
PublisherHumana Press Inc.
Pages47-62
Number of pages16
DOIs
StatePublished - Jan 1 2018

Publication series

NameMethods in Molecular Biology
Volume1703
ISSN (Print)1064-3745

Fingerprint

DNA Topoisomerases
Fluoroquinolones
Topoisomerase Inhibitors
Anti-Bacterial Agents
Topoisomerase I Inhibitors
Quinolones
Drug Delivery Systems
Drug Resistance
Pharmaceutical Preparations
Bacteria

Keywords

  • Aminocoumarin
  • Antibacterial drugs
  • DNA gyrase
  • Fluoroquinolone
  • Topoisomerase I
  • Topoisomerase IV
  • Topoisomerase poison

Cite this

Hiasa, H. (2018). DNA topoisomerases as targets for antibacterial agents. In Methods in Molecular Biology (pp. 47-62). (Methods in Molecular Biology; Vol. 1703). Humana Press Inc.. DOI: 10.1007/978-1-4939-7459-7_3

DNA topoisomerases as targets for antibacterial agents. / Hiasa, Hiroshi.

Methods in Molecular Biology. Humana Press Inc., 2018. p. 47-62 (Methods in Molecular Biology; Vol. 1703).

Research output: Chapter in Book/Report/Conference proceedingChapter

Hiasa, H 2018, DNA topoisomerases as targets for antibacterial agents. in Methods in Molecular Biology. Methods in Molecular Biology, vol. 1703, Humana Press Inc., pp. 47-62. DOI: 10.1007/978-1-4939-7459-7_3
Hiasa H. DNA topoisomerases as targets for antibacterial agents. In Methods in Molecular Biology. Humana Press Inc.2018. p. 47-62. (Methods in Molecular Biology). Available from, DOI: 10.1007/978-1-4939-7459-7_3
Hiasa, Hiroshi. / DNA topoisomerases as targets for antibacterial agents. Methods in Molecular Biology. Humana Press Inc., 2018. pp. 47-62 (Methods in Molecular Biology).
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