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. 2010 Sep;17(9):1152-3.
doi: 10.1038/nsmb.1892. Epub 2010 Aug 29.

Structural basis of quinolone inhibition of type IIA topoisomerases and target-mediated resistance

Alexandre Wohlkonig  1 , Pan F Chan, Andrew P Fosberry, Paul Homes, Jianzhong Huang, Michael Kranz, Vaughan R Leydon, Timothy J Miles, Neil D Pearson, Rajika L Perera, Anthony J Shillings, Michael N Gwynn, Benjamin D Bax
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Structural basis of quinolone inhibition of type IIA topoisomerases and target-mediated resistance

Alexandre Wohlkonig et al. Nat Struct Mol Biol. 2010 Sep.

Abstract

Quinolone antibacterials have been used to treat bacterial infections for over 40 years. A crystal structure of moxifloxacin in complex with Acinetobacter baumannii topoisomerase IV now shows the wedge-shaped quinolone stacking between base pairs at the DNA cleavage site and binding conserved residues in the DNA cleavage domain through chelation of a noncatalytic magnesium ion. This provides a molecular basis for the quinolone inhibition mechanism, resistance mutations and invariant quinolone antibacterial structural features.

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