Mechanism of inhibition of DNA gyrase by cyclothialidine, a novel DNA gyrase inhibitor.

摘要: Abstract We investigated how cyclothialidine (Ro 09-1437), a novel DNA gyrase inhibitor belonging to new chemical class of compounds, acts inhibit Escherichia coli gyrase. Cyclothialidine up 100 micrograms/ml showed no effect on when linear was used as substrate. Under the same conditions, quinolones, which resealing reaction gyrase, caused decrease in amount used. No observed accumulation covalent complex and A subunit induced by ofloxacin absence ATP. The supercoiling antagonized ATP, reducing inhibitory activity 11-fold ATP concentration increased from 0.5 5 mM. competitively inhibited ATPase (Ki = 6 nM). binding [14C]benzoyl-cyclothialidine E. novobiocin, but not ofloxacin. These results suggest that interfering with B active against resistant suggesting its precise site action might be different novobiocin.