Target proteins docked were DNA gyrase
, topoisomerase-IV of the bacteria, lanosterol 14-alpha-demethylase of the fungi, cycloxygenase-2 (Cox-2) and epidermal growth factor receptor tyrosine kinase (EGFR.
Synthesis, Characterization, Antioxidant, Antimicrobial, Cytotoxic, Anticancer, Leishmanicidal, Anti-inflammatory Activities and Docking Studies of Heterocyclic 1,3,4-oxadiazoles and 4-amino-1,2,4-triazoles Derivatives
Effect of differen classes of inhibitors on DNA gyrase
from Mycobacterium smegmatis.
High-level fluoroquinolone resistance in Pseudomonas aeruginosa due to interplay of the MexAB-OprM efflux pump and the DNA gyrase
The superhelical state of intracellular DNA is regulated by the actions of DNA gyrase
and topoisomerase I, which removes DNA super helical twists but is not inhibited by quinolones.
is essential for bacteria and plants but is not present in animals or humans.
Reduced susceptibility to the fluoroquinolones group of antibiotics is usually linked with point mutations in the bacterial target genes gyrA, gyrB encoding DNA gyrase
and/or parC, parE encoding DNA topoisomerase IV.
A recent example is the direct relation between the DNA gyrase
functional mode of action and the applied mechanical stress (1).
leprae is unknown, but in other bacteria it appears to inhibit DNA replication by inactivating the DNA gyrase
, a tetramer containing two [beta]-subunits (GyrA) and two [beta]-subunits (GyrB).
Identification of pathogenic Leptospira species by conventional or real-time PCR and sequencing of the DNA gyrase
subunit B encoding gene.
Specifically, they inhibit the activity of DNA gyrase
and topoisomerase IV.
It functions by inhibiting DNA gyrase
, a type II topoisomerase, which is an enzyme necessary to separate replicated DNA, thereby inhibiting cell division.
Quinolones have a bactericidal effect when these bind with two target enzymes, DNA gyrase
and topoisomerase IV, which are essential for DNA replication within the cell.
With detailed methods and protocols, contributors address computational strategies, a number of assay methods (for DNA gyrase
, topoisomerase IV, bacterial RNA polymerase, bacterial ribosome biogenesis and inhibitors targeting specific translational steps), high-throughput peptide deformylase inhibitor screening, penicillin-binding protein assay methods, methods for assessing the structure and function of cationic antimicrobial peptides, and bacterial efflux pump inhibitors.
catalyses the negative supercoiling of DNA in bacteria and consists of two A subunits, encoded by gyrA, and two B subunits, encoded by gyrB.
Ohemeng and colleagues previously detected no inhibitory activity from galangin against Escherichia coli DNA gyrase
(Ohemeng et al.