What drugs inhibit DNA gyrase?
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.
Which antibiotics act on DNA gyrase?
Fluoroquinolones have been the most successful antibacterial agents targeting DNA gyrase. These compounds have been extensively explored and researched to improve spectrum of activity, potency and bacterial resistance.
Why do quinolones not target human host?
No harm comes to the human host because penicillin does not inhibit any biochemical process that goes on within us. Bacteria can also be selectively eradicated by targeting their metabolic pathways. Both bacteria and humans carry out protein synthesis on structures called ribosomes.
What group of antibiotics interferes with the DNA replicating enzyme DNA gyrase?
Quinolones are a key group of antibiotics that interfere with DNA synthesis by inhibiting topoisomerase, most frequently topoisomerase II (DNA gyrase), an enzyme involved in DNA replication.
Does ciprofloxacin bind to DNA gyrase?
Ciprofloxacin and other quinolone drugs are known to bind bacterial DNA gyrase and cause it to introduce double-stranded breaks into DNA (30, 31); this is thought to be a lethal event in vivo (32). This mechanism of cell killing results in dominance of a quinolone-sensitive gyrA over a resistant allele (33).
Does tetracycline have penicillin in it?
by Drugs.com Tetracyclines are unrelated to penicillins and therefore are safe to take in hypersensitive patients. Other unrelated antibiotics include quinolones (e.g. ciprofloxacin), macrolides (e.g. clarithromycin), aminoglycosides (e.g. gentamicin) and glycopeptides (e.g. vancomycin).
What does gyrase do in bacteria?
DNA gyrase is an essential bacterial enzyme that catalyzes the ATP-dependent negative super-coiling of double-stranded closed-circular DNA. Gyrase belongs to a class of enzymes known as topoisomerases that are involved in the control of topological transitions of DNA.
What is DNA gyrase responsible for?
How do quinolones inhibit DNA gyrase?
Quinolones dually target DNA gyrase and topoisomerase IV binding to specific domains and conformations so as to block DNA strand passage catalysis and stabilize DNA–enzyme complexes that block the DNA replication apparatus and generate double breaks in DNA that underlie their bactericidal activity.