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Efflux pump inhibitors: new updates
Pharmacological Reports, 2020The discovery of antibiotics ought to have ended the issue of bacterial infections, but this was not the case as it has led to the evolution of various mechanisms of bacterial resistance against various antibiotics. The efflux pump remains one of the mechanisms through which organisms develop resistance against antibiotics; this is because organisms ...
Manaf AlMatar +3 more
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New-generation efflux pump inhibitors
Expert Review of Clinical Pharmacology, 2008The development of novel efflux pump inhibitors is an emerging and challenging research field. Besides the use of such excipients in cancer therapy, efflux pump inhibitors are gaining increasing interest with regards to drug delivery. In particular, inhibition of efflux pumps located in the intestine and the blood-brain barrier offers promising ...
Martin, Werle +2 more
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Efflux pump inhibitors in bacteria
Expert Opinion on Therapeutic Patents, 2007The efficacy of antibiotherapy of infectious diseases is strongly compromised by the advent and spread of antibiotic resistance. Active efflux of cytotoxic drugs mediated by multi-drug transporters is the basis of multi-drug resistance in prokaryotic cells.
Sandrine Alibert, Jean-Marie Pagès
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Computational modelling of efflux pumps and their inhibitors [PDF]
Essays in Biochemistry, 2017 Antimicrobial resistance is based on the multifarious strategies that bacteria adopt to face antibiotic therapies, making it a key public health concern of our era. Among these strategies, efflux pumps (EPs) contribute significantly to increase the levels and profiles of resistance by expelling a broad range of unrelated compounds – buying time for the
RAMASWAMY, VENKATA KRISHNAN +4 more
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Bacterial Efflux Pump Inhibitors
2008Infections caused by multidrug-resistant Gram-negative pathogens play a major role in the morbidity and mortality of hospitalized patients. The rise of resistance to current antibiotic therapies has made the discovery of new agents urgent. One of the major antibiotic resistance mechanisms utilized by more than 15 species of Gram-negative bacterial ...
Barbara J, Kamicker +7 more
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Bacterial efflux systems and efflux pumps inhibitors
Biochimie, 2005It is now well established that bacterial resistance to antibiotics has become a serious problem of public health that concerns almost all antibacterial agents and that manifests in all fields of their application. Among the three main mechanisms involved in bacterial resistance (target modification, antibiotic inactivation or default of its ...
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An Overview of Bacterial Efflux Pumps and Computational Approaches to Study Efflux Pump Inhibitors
Future Medicinal Chemistry, 2016Micro-organisms express a wide range of transmembrane pumps known as multidrug efflux pumps that improve the micro-organism's ability to survive in severe environments and contribute to resistance against antibiotic and antimicrobial agents. There is significant interest in developing efflux inhibitors as an adjunct to treatment with current and next ...
Jamshidi, Shirin +2 more
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Inhibitors of efflux pumps in Gram-negative bacteria
Trends in Molecular Medicine, 2005In Gram-negative bacteria, efflux complexes, consisting of an inner-membrane pump, a periplasmic adaptor protein and outer-membrane channel, provide an efficient means for the export of structurally unrelated drugs, causing the multidrug-resistance phenotype. Resistance due to this antibiotic efflux is an increasing problem worldwide.
Jean-Marie, Pagès +2 more
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Antimicrobial Drug Efflux Pump Inhibitors
2016Bacterial multidrug resistance is on the rise, and bacterial efflux pumps make a major contributor to this development. Efflux pump inhibitors (EPIs) may be a solution to this problem, since they can reverse resistance to clinically administered antimicrobial agents. Multiple EPIs with activity against Gram-positive and Gram-negative bacteria have been
Jürgen A. Bohnert, Winfried V. Kern
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Development of efflux pump inhibitors in antituberculosis therapy
International Journal of Antimicrobial Agents, 2016Resistance and tolerance to antituberculosis (anti-TB) drugs, especially the first-line drugs, has become a serious problem in anti-TB therapy. Efflux of antimicrobial agents via bacterial efflux pumps is one of the main reasons for drug resistance.
Lele, Song, Xueqiong, Wu
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