Effect of different classes of inhibitors on DNA gyrase from Mycobacterium smegmatis.


Journal Article

Quinolones, coumarins, cyclothialidines, CcdB and microcin B17 inhibit DNA gyrase. Information regarding these various inhibitors comes from studies performed with the enzyme from Escherichia coli, and subsequent analyses have also primarily been confined to this system. We have carried out a detailed analysis of the effect of various groups of inhibitors on Mycobacterium smegmatis gyrase and demonstrate differential susceptibility of the E. coli and M. smegmatis gyrases. Interestingly, M. smegmatis gyrase was refractory to the plasmid-borne proteinaceous inhibitors CcdB and microcin B17. Ciprofloxacin, a fluoroquinolone, showed a 10-fold reduction in efficacy against M. smegmatis compared with E. coli gyrase. We have also shown that etoposide, an antineoplastic drug, inhibits DNA gyrase activity by trapping the gyrase-DNA complex. DNA gyrases from both E. coli and M. smegmatis were susceptible to etoposide at comparable levels.

Full Text

Cited Authors

  • Chatterji, M; Unniraman, S; Mahadevan, S; Nagaraja, V

Published Date

  • October 1, 2001

Published In

Volume / Issue

  • 48 / 4

Start / End Page

  • 479 - 485

PubMed ID

  • 11581225

Pubmed Central ID

  • 11581225

Electronic International Standard Serial Number (EISSN)

  • 1460-2091

International Standard Serial Number (ISSN)

  • 0305-7453

Digital Object Identifier (DOI)

  • 10.1093/jac/48.4.479


  • eng