منابع مشابه
Quinolones: Action and Resistance Updated
The quinolones trap DNA gyrase and DNA topoisomerase IV on DNA as complexes in which the DNA is broken but constrained by protein. Early studies suggested that drug binding occurs largely along helix-4 of the GyrA (gyrase) and ParC (topoisomerase IV) proteins. However, recent X-ray crystallography shows drug intercalating between the -1 and +1 nucleotides of cut DNA, with only one end of the dr...
متن کاملMechanism of action of and resistance to quinolones
Fluoroquinolones are an important class of wide-spectrum antibacterial agents. The first quinolone described was nalidixic acid, which showed a narrow spectrum of activity. The evolution of quinolones to more potent molecules was based on changes at positions 1, 6, 7 and 8 of the chemical structure of nalidixic acid. Quinolones inhibit DNA gyrase and topoisomerase IV activities, two enzymes ess...
متن کاملTrastuzumab: Updated Mechanisms of Action and Resistance in Breast Cancer
HER2-positive breast cancer accounts for 20-30% of all breast cancers and has the second-poorest prognosis among breast cancer subtypes. The approval of trastuzumab in 1998 has significantly improved patients' outcomes and paved the way for the beginning of advent of targeted approaches in breast cancer treatment. However, primary or acquired resistance to trastuzumab has been increasingly reco...
متن کاملResistance to quinolones in mycobacteria.
Ohno, H., Koga, H., Kohno, S.. Higashiyama, Y., Miyazaki, Y., Ogawa, K., Yanagihra, K., Yamamoto, Y., Noda, T. & Miyamoto, J. (1994), Evaluation for rapid detection of rifampiein-rcsistant MycobacteHum tuberculosis by polymerase chain reaction-single strand conformation polymorphism. Kekkaku, 69, 773-778. Predieh, M., Doukhan, L., Nair, G. & Smith, I. (1995), Characterization of RNA polymerase ...
متن کاملMechanisms of resistance to quinolones.
The increased use of fluoroquinolones has led to increasing resistance to these antimicrobials, with rates of resistance that vary by both organism and geographic region. Resistance to fluoroquinolones typically arises as a result of alterations in the target enzymes (DNA gyrase and topoisomerase IV) and of changes in drug entry and efflux. Mutations are selected first in the more susceptible t...
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ژورنال
عنوان ژورنال: Current Topics in Medicinal Chemistry
سال: 2009
ISSN: 1568-0266
DOI: 10.2174/156802609789630947