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Shiou-Ling Lu. Quinolone. Quinolones are potent antibacterial agents that specifically target bacterial DNA gyrase and topoisomerase IV. Previous studies have shown that quinolone resistance arises by mutations in chromosomal genes .

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quinolone
Quinolone
  • Quinolones are potent antibacterial agents that specifically target bacterial DNA gyrase and topoisomerase IV.
  • Previous studies have shown that quinolone resistance arises by mutations in chromosomal genes.
  • Recently, a multiresistance plasmid was discovered that encodes transferable resistance to quinolones.

Gram negative bacteria

Quinolone

Resistant

DNA gyrase

topoisomerase IV

slide3
The plasmid-quinolone resistance gene, qnr. and found it in an integron-like environment upstream from qacE1 and sulI.
slide4
The gene product Qnr was a 218-aa protein belonging to the pentapeptide repeat family and shared sequence homology with the immunity protein McbG, which is thought to protect DNA gyrase from the action of microcin B17. Qnr had pentapeptide repeat domains of 11 and 28 tandem copies.
slide5

Supercoild DNA + + + + + +

DNA gyrase - + + + + +

Ciprofloxacin - - + + + +

Qnr - - - 2 mM 1mM -

Ciprofloxacin

Quinolone

Qnr

DNA gyrase

slide6

Qnr

Ciprofloxacin

Quinolone

Qnr

DNA gyrase

slide7

Ciprofloxacin vs. Qnr

Qnr : 2 mM

Ciprofloxacin

0.75 mM

1.5 mM

3 mM

6 mM

Ciprofloxacin

Quinolone

Qnr

DNA gyrase

v

v

v

slide8

Gyrase

0.62 nM

0.31 nM

0.93 nM

Qnr

Qnr

Qnr

Qnr

DNA gyrase

slide9

Quinolone

Qnr

DNA gyrase

topoisomerase IV

slide10

Resistant

Gram negative bacteria

Quinolone

Qnr

DNA gyrase

topoisomerase IV