Fig. 5: LEI-800 is an exceptionally strong supercoiling inhibitor.
a, A schematic representation of negative supercoiling. In a supercoiling assay, relaxed (R) DNA is transformed into supercoiled (SC) DNA by DNA gyrase. b, Three compounds tested for supercoiling inhibition. CIP (blue) is used as positive control, LEI-801 (coral) is used as antimicrobially inactive compound and LEI-800 (gold) is used as lead compound. c, Dose-response curves of DNA gyrase supercoiling inhibition, based on n = 3 gels. The mean is shown with error bars and dotted lines representing the standard deviation at each concentration and the 95% confidence interval (CI), respectively. d, Representative agarose gels for E. coli DNA gyrase supercoiling inhibition by the three compounds. e, Checkerboard broth microdilution assays show pharmacological disruption of LPS by PMBN does not have an effect on the antimicrobial activity of CIP, yet potentiates both LEI-801 and LEI-800.
