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

@article{Wohlkonig2010StructuralBO,
  title={Structural basis of quinolone inhibition of type IIA topoisomerases and target-mediated resistance},
  author={Alexandre Wohlkonig and Pan F. Chan and Andrew P. Fosberry and Paul Homes and Jianzhong Huang and Michael Kranz and Vaughan R. Leydon and Timothy J Miles and Neil David GlaxoSmithKline Pearson and Rajika L Perera and Anthony Shillings and Michael N. Gwynn and Benjamin D. Bax},
  journal={Nature Structural \&Molecular Biology},
  year={2010},
  volume={17},
  pages={1152-1153}
}
  • A. Wohlkonig, P. Chan, +10 authors B. Bax
  • Published 1 September 2010
  • Biology, Chemistry, Medicine
  • Nature Structural &Molecular Biology
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… Expand
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