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New-generation efflux pump inhibitors

Expert Review of Clinical Pharmacology, 2008
The 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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Leishmaniasis: efflux pumps and chemoresistance

International Journal of Antimicrobial Agents, 2003
Resistance of parasitic protozoa such as Leishmania to therapeutic drugs continues to escalate in developing countries. Treatment programs for human leishmaniasis are still based on pentavalent antimonials but resistance to these compounds has been a persistent problem.
Clara, Leandro, Lenea, Campino
openaire   +2 more sources

Bacterial Efflux Pump Inhibitors

2008
Infections 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
openaire   +2 more sources

Bacterial efflux systems and efflux pumps inhibitors

Biochimie, 2005
It 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 ...
openaire   +2 more sources

Mycobacterial efflux pumps and chemotherapeutic implications

International Journal of Antimicrobial Agents, 2003
The demonstration of the existence of active efflux pumps in mycobacteria raises the question of whether or not these can increase in number and activity rendering wild-type mycobacteria increasingly resistant to a given antibiotic. This could be a mechanism by which mutated resistant strains become better fit to the selective environment ...
Miguel, Viveiros   +2 more
openaire   +2 more sources

An Overview of Bacterial Efflux Pumps and Computational Approaches to Study Efflux Pump Inhibitors

Future Medicinal Chemistry, 2016
Micro-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
openaire   +3 more sources

Efflux pumps and mutation

Science, 2018
Antibiotic Resistance Antibiotic resistance is an alarming and growing challenge. Bacteria show great heterogeneity in growth and mutation rates. Such variability allows some cells to persist during transient antibiotic exposure. During this persistent phase, mutations accumulate, which can result in selection for full-blown antibiotic resistance.
openaire   +1 more source

Efflux pump inhibitors in bacteria

Expert Opinion on Therapeutic Patents, 2007
The 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
openaire   +1 more source

Multidrug Efflux Pumps in the Genus Erwinia: Physiology and Regulation of Efflux Pump Gene Expression

2016
Plant pathogens belonging to the genus Erwinia cause diseases in several economically important plants. Plants respond to bacterial infection with a powerful chemical arsenal and signaling molecules to rid themselves of the microbes. Although our understanding of how Erwinia initiate infections in plants has become clear, a comprehensive understanding ...
J, Thekkiniath   +2 more
openaire   +2 more sources

Inhibitors of Efflux Pumps

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
openaire   +1 more source

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