Molecular Classification
Enzyme, Topoisomerase, Type II Topoisomerase
Other Names
Gyrase, DNA topoisomerase (ATP-hydrolyzing)
Disease Roles
Infection

DNA Gyrase Overview

DNA gyrase is an essential bacterial enzyme classified as a type II topoisomerase. Its primary function is to introduce negative supercoils into double-stranded closed-circular DNA in an ATP-dependent manner. This activity is crucial for maintaining the proper topology of bacterial DNA, which facilitates processes such as replication and transcription by relieving torsional strain generated during these events. It is a validated antibacterial target.

Mechanism of Action

Inhibition of DNA gyrase activity by blocking strand cleavage/religation or ATP binding/hydrolysis, leading to accumulation of double-strand breaks and/or failure to resolve topological stress during replication/transcription.

Biological Functions

DNA supercoiling
DNA relaxation
DNA catenation
DNA decatenation
Chromosome condensation
Transcription initiation
Replication origin firing
Maintenance of chromosome structure

Disease Associations

Infection

Safety Considerations

  • Development of bacterial resistance
  • Off-target effects of inhibitors

Interacting Drugs

Quinolones
Ciprofloxacin
Coumarins
Aminocoumarins