Target intelligence / Profile preview

Bacterial DNA gyrase (Type II topoisomerase) (DNA gyrase)

Target
DNA gyrase
Molecular classification
Enzyme, Type II topoisomerase
01

Overview

Bacterial DNA gyrase is a specialized Type II topoisomerase enzyme found exclusively in bacteria, composed of GyrA and GyrB subunits. It is unique in its ability to introduce negative supercoils into DNA using ATP hydrolysis, in addition to relaxing positive supercoils. By actively managing DNA supercoiling, DNA gyrase facilitates, and is essential for, DNA replication, transcription, and maintenance of chromosome structure. DNA gyrase is a validated and widely exploited antibacterial drug target; its inhibition leads to the accumulation of DNA breaks and bacterial cell death. Structurally and functionally, gyrase differs from eukaryotic topoisomerases, making it a selective target for antibiotics such as fluoroquinolones and coumarins.

Other names
DNA topoisomerase IIGyrase (GyrA/GyrB)Type II DNA topoisomeraseTopoisomerase II (bacterial)Gyrase AGyrase B
02

Mechanism of action

Drugs bind to the gyrase-DNA complex, stabilizing the DNA cleavage state and preventing religation, leading to double-strand DNA breaks and bacterial cell death (bactericidal effect). Inhibition of ATPase activity, blocking energy-dependent supercoiling.

03

Biological functions

Regulation of DNA supercoilingRelaxation of positive DNA supercoilsIntroduction of negative DNA supercoilsResolution of DNA topology during replication and transcription
04

Disease associations

Infection (primarily bacterial infections targeted by antibiotics)
05

Safety considerations

Target is bacterial-specific, so drugs are generally selective, but off-target toxicity can arise from effects on mitochondrial topoisomerases or gut flora disruption.Resistance development due to target mutations (notably in gyrA/gyrB)Rare hypersensitivity reactions to quinolone drugs
06

Interacting drugs

Quinolones (e.g., ciprofloxacin, levofloxacin)

4 more in the full profile.

07

Biomarkers

Mutations in gyrA and gyrB genes (linked to antibiotic resistance, particularly to fluoroquinolones)

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