Table 6. Interference with the Action of DNA Processing Enzymes by MGB-BP-3.
S. aureus |
E. coli |
|||
---|---|---|---|---|
enzyme | MGB-BP-3 | fluoroquinolonea | MGB-BP-3 | fluoroquinolonea |
gyrase supercoiling IC50 (μM) | 1.94 | 14.81 | 6.00 | 0.34 |
fluoroquinolone-resistantb gyrase supercoiling IC50 (μM) | 3.04 | 338.27 | 8.17 | 8.84 |
gyrase cleavage CC50 (μM) | >500 | 3.22 | >500 | 0.29 |
Topo IV decatenation IC50 (μM) | 2.50 | 7.69 | 1.93 | 1.82 |
Topo IV relaxation IC50 (μM) | 2.02 | 0.86 | 1.98 | 2.44 |
Topo IV cleavage CC50 (μM) | >500 | 6.2 | >500 | 6.2 |
Ciprofloxacin control for all assays except the cleavage assays for which norfloxacin was used.
S83L gyrase for S. aureus and S84L gyrase for E. coli.