Mechanism of fluoroquinolone action.
When fluoroquinolones bind to gyrase or topoisomerase IV in the presence of DNA, they alter protein conformation. DNA cleavage results with diminished religation, so the enzymes are trapped in ternary complexes with drug and cleaved DNA. Preferential localization of gyrase ahead of replication forks and topoisomerase IV behind them causes fluoroquinolone-mediated complexes with the two enzymes to have different physiological consequences.
Drlica
K
K
Public Health Research Institute 455 First Avenue, New York, NY 10016, USA. drlica@phri.nyu.edu.
D000890:Anti-Infective Agents / Q000378:metabolism* / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects* / Q000201:enzymology; D027101:DNA Topoisomerase IV; D004250:DNA Topoisomerases, Type II / Q000378:metabolism*; D004269:DNA, Bacterial / Q000378:metabolism; D004352:Drug Resistance, Microbial; D024841:Fluoroquinolones
D000890:Anti-Infective Agents; D004269:DNA, Bacterial; D024841:Fluoroquinolones; D027101:DNA Topoisomerase IV; D004250:DNA Topoisomerases, Type II