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Mechanism of Drug Resistance in Staphylococcus aureus and Future Drug Discovery
Published in Peter Grunwald, Pharmaceutical Biocatalysis, 2020
Felipe Wakasuqui, Ana Leticia Gori Lusa, Sven Falke, Christian Betzel, Carsten Wrenger
Quinolones are broad-spectrum antibiotic related to the compound 4-quinolone. Quinolones act on the type II topoisomerases, topoisomerase IV, and DNA gyrase, all enzymes which physiologically break and repair DNA to prevent coiling tension, turning them into lethal enzymes which fragment the DNA by stabilizing the cleavage complexes and preventing DNA ligation (Aldred et al., 2014). Both enzymes are heterotetramers, composed of two subunits, A and B, and resistance is commonly due to mutations in these subunits (Tanaka et al., 2000), especially identified for a serine residue that anchors a water - metal ion bridge (Aldred et al., 2014). S. aureus also contains in its genome genes for a multidrug resistance membrane bound efflux pump, which provides resistance to fluoroquinolones, as the norA gene (Kaatz et al., 1993), and norB and norC genes (Truong-Bolduc et al., 2006).
Effects of ciprofloxacin on biogas production and microbial community composition in anaerobic digestion of swine wastewater in ASBR type reactor
Published in Environmental Technology, 2023
José Gustavo Venâncio da Silva Ramos, Camila Palacio Richter, Maria Alice Silva, Giordana Longo Singolano, Gabriel Hauagge, Eduarda Lorençon, Ismael Laurindo Costa Junior, Thiago Edwiges, Priscila Vaz de Arruda, Carlos Magno de Sousa Vidal
In this context, we can mention ciprofloxacin (CIP), one of the most used antibiotics in the swine industry [7,8]. Fluoroquinolones – the ciprofloxacin group – are used for Gram-negative bacilli and have good activity against some Gram-positive cocci. These drugs inhibit the activity of DNA gyrase and topoisomerase IV, essential enzymes for bacterial survival. DNA gyrase makes the DNA molecule compact and biologically active through the introduction of super-helical twists, while DNA topoisomerase IV is responsible for removing the interconnection between daughter chromosomes, allowing the separation of the two daughter cells at the end of the replication cycle. The drug action causes the death of the pathogenic microorganisms [9,10].