Target intelligence / Profile preview

Bacterial DNA gyrase–DNA complex (DNA gyrase)

Target
DNA gyrase
Molecular classification
Enzyme, Type II topoisomerase, Protein-nucleic acid complex
01

Overview

The Bacterial DNA gyrase–DNA complex is a critical intermediate in the catalytic cycle of DNA gyrase, an essential type II topoisomerase found in bacteria (PubMed: 10640677). This complex is formed when the heterotetrameric enzyme, consisting of GyrA and GyrB subunits, binds to and cleaves double-stranded DNA to introduce negative supercoils (UniProt: P0AES4). This process is fundamental for relieving torsional strain during DNA replication and transcription, ensuring the bacterial genome remains accessible and functional (StatPearls: NBK547665). The complex is the primary pharmacological target for fluoroquinolone antibiotics, which bind at the interface of the enzyme and the DNA (PubChem: CID 2764). By stabilizing this 'cleavage complex,' the drugs prevent the religation of the DNA strands, effectively converting the enzyme into a cellular toxin that generates permanent double-strand breaks (PubMed: 21696353). The clinical effectiveness of targeting this complex is frequently compromised by mutations in the GyrA or GyrB subunits that reduce drug affinity, leading to widespread antibiotic resistance (PubMed: 12654733).

Other names
Type II topoisomeraseGyrA-GyrB complexDNA topoisomerase IIGyrase-DNA complex
02

Mechanism of action

Stabilization of the covalent enzyme-DNA cleavage complex, preventing DNA religation and inducing double-strand breaks.

03

Biological functions

DNA supercoilingDNA replicationDNA transcriptionChromosome decatenation
04

Disease associations

Infection
05

Safety considerations

Antimicrobial resistanceTendonitis and tendon rupturePeripheral neuropathyCentral nervous system toxicityQT interval prolongation
06

Interacting drugs

Ciprofloxacin

7 more in the full profile.

07

Biomarkers

Minimum Inhibitory Concentration (MIC)GyrA gene mutationsGyrB gene mutations

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