Exploiting bacterial DNA gyrase as a drug target: current state and perspectives

Appl Microbiol Biotechnol. 2011 Nov;92(3):479-97. doi: 10.1007/s00253-011-3557-z. Epub 2011 Sep 9.


DNA gyrase is a type II topoisomerase that can introduce negative supercoils into DNA at the expense of ATP hydrolysis. It is essential in all bacteria but absent from higher eukaryotes, making it an attractive target for antibacterials. The fluoroquinolones are examples of very successful gyrase-targeted drugs, but the rise in bacterial resistance to these agents means that we not only need to seek new compounds, but also new modes of inhibition of this enzyme. We review known gyrase-specific drugs and toxins and assess the prospects for developing new antibacterials targeted to this enzyme.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Adenosine Triphosphate / metabolism
  • Anti-Bacterial Agents / metabolism*
  • Bacteria / drug effects*
  • Bacteria / enzymology*
  • DNA, Bacterial / metabolism*
  • Models, Biological
  • Models, Molecular
  • Quinolones / metabolism
  • Topoisomerase II Inhibitors*


  • Anti-Bacterial Agents
  • DNA, Bacterial
  • Quinolones
  • Topoisomerase II Inhibitors
  • Adenosine Triphosphate