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Mycobacterial DNA Gyrase (Gyrase)
- Target
- Gyrase
- Molecular classification
- Enzyme, Type II topoisomerase
01
Overview
Mycobacterial DNA gyrase is a type II topoisomerase enzyme essential for DNA topology maintenance in mycobacteria, including Mycobacterium tuberculosis. It is a heterotetramer (A2B2) that introduces negative supercoils into DNA, critical for replication, transcription, and chromosome segregation. It is a validated drug target for anti-tubercular agents, including fluoroquinolones and novel Mycobacterial Gyrase Inhibitors (MGIs).
- Other names
- DNA gyraseGyrA2B2Mycobacterium tuberculosis DNA gyrase
02
Mechanism of action
Inhibition of DNA gyrase activity, leading to DNA damage and cell death. Fluoroquinolones stabilize the cleavage complex leading to double stranded breaks. MGIs induce single-stranded breaks.
03
Biological functions
DNA supercoilingDNA relaxationDNA decatenationDNA unknottingDNA replicationTranscription
04
Disease associations
Infection
05
Safety considerations
Resistance development through mutations in gyrA and gyrB genesPotential for off-target effects
06
Interacting drugs
Fluoroquinolones (e.g., moxifloxacin)
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