title: Exploiting bacterial DNA gyrase as a drug target: current state and perspectives.
abstract: 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.
authors: Department Biological Chemistry, John Innes Centre, Norwich Research Park, Norwich, NR4 7UH, UK.
authors: Frédéric
authors: F
authors: Collin
authors: Shantanu
authors: S
authors: Karkare
authors: Anthony
authors: A
authors: Maxwell
mesh_terms: D000255:Adenosine Triphosphate / Q000378:metabolism; D000900:Anti-Bacterial Agents / Q000378:metabolism*; D001419:Bacteria / Q000187:drug effects* / Q000201:enzymology*; D004269:DNA, Bacterial / Q000378:metabolism*; D008954:Models, Biological; D008958:Models, Molecular; D015363:Quinolones / Q000378:metabolism; D059005:Topoisomerase II Inhibitors
chemical_list: D000900:Anti-Bacterial Agents; D004269:DNA, Bacterial; D015363:Quinolones; D059005:Topoisomerase II Inhibitors; D000255:Adenosine Triphosphate