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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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N-Caffeoylphenalkylamide derivatives as bacterial efflux pump inhibitors
Bioorganic & Medicinal Chemistry Letters, 2007As part of an ongoing project to identify plant natural products as efflux pump inhibitors (EPIs), bioassay-guided fractionation of the methanolic extract of Mirabilis jalapa Linn. (Nyctaginaceae) led to the isolation of an active polyphenolic amide: N-trans-feruloyl 4'-O-methyldopamine.
Michalet, Serge +7 more
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An Update on Staphylococcus aureus NorA Efflux Pump Inhibitors
Current Topics in Medicinal Chemistry, 2020Background: Methicillin-resistant and vancomycin-resistant Staphylococcus aureus are pathogens causing severe infectious diseases that pose real public health threats problems worldwide. In S. aureus, the most efficient multidrug-resistant system is the NorA efflux pump. For this reason, it is critical to identify efflux pump inhibitors. Objective:
Kadja Luana Chagas, Monteiro +2 more
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Efflux pump inhibitors reduce the invasiveness of Pseudomonas aeruginosa
International Journal of Antimicrobial Agents, 2009Efflux systems are thought to contribute to antimicrobial resistance in Pseudomonas aeruginosa. The mexAB-oprM deletion strain of P. aeruginosa PAO1 is compromised in its capacity to invade Madin-Darby canine kidney (MDCK) cells, suggesting that P. aeruginosa exports invasion determinants using a MexAB-OprM system.
Yoichi, Hirakata +11 more
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Multidrug-resistant bacteria are a major public health threat. MDR efflux pump overexpression and enzymatic changes are major antibiotic resistance mechanisms. Many drug and biofilm resistance strategies involve efflux pumps. Natural substrate and inhibitor identification is a new study. Efflux pump inhibition allows medication buildup inside bacterial
Neeraj Kumar +2 more
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Neeraj Kumar +2 more
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