Fluoroquinolone-gyrase-DNA complexes two modes of drug binding

Arkady Mustaev, Muhammad Malik, Xilin Zhao, Natalia Kurepina, Gan Luan, Lisa M. Oppegard, Hiroshi Hiasa, Kevin R. Marks, Robert J. Kerns, James M. Berger, Karl Drlica

Research output: Contribution to journalArticlepeer-review

81 Scopus citations


Background: X-ray crystal structures of fluoroquinolone-gyrase-DNA complexes reveal a single drug-binding mode. Results: A ciprofloxacin derivative with a chloroacetyl moiety at the C-7 end cross-linked with cysteine substitutions in both GyrA and GyrB that were 17 A apart. Conclusion: Cleaved complexes containing gyrase have two fluoroquinolone-binding modes. Significance: The additional drug-binding mode provides new ways to investigate inhibitor-topoisomerase interactions.

Original languageEnglish (US)
Pages (from-to)12300-12312
Number of pages13
JournalJournal of Biological Chemistry
Issue number18
StatePublished - 2014

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Cell Biology


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