JAC Advance Access originally published online on April 14, 2003
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Journal of Antimicrobial Chemotherapy (2003) 51, 1067-1077
© 2003 The British Society for Antimicrobial Chemotherapy
Leading Article |
Antibiotic efflux pumps in eukaryotic cells: occurrence and impact on antibiotic cellular pharmacokinetics, pharmacodynamics and toxicodynamics
Unité de Pharmacologie Cellulaire et Moléculaire, Université Catholique de Louvain, 73.70 avenue Mounier 73, B-1200 Brussels, Belgium
Keywords: antibiotics, efflux, transporters, eukaryotes, influx
| The first 150 words of the full text of this article appear below. |
Active efflux is now recognized as a key element in drug disposition and activity. Original observations were first limited to a few compounds examined in specific situations, such as anthracyclines in the context of resistance of cancer cells, and tetracyclines in the context of bacterial resistance. However, the combination of systematic surveys involving commonly used drugs and genome sequencing has identified 
20 families of drug transporters.1 Many of them are ubiquitous, and are expressed in prokaryotes and archaea as well as in inferior and superior eukaryotes. A companion review2 deals with antibiotic transporters in prokaryotes, where we examine their role and impact on intrinsic antimicrobial activity and resistance. We concentrate here on eukaryotic cells in general, and on animals (including man) in particular, to show how transporters need to be taken into account for a proper understanding as to how antibiotics are handled in vivo.
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Why are antibiotics transported in eukaryotic cells? |
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In general, drug transporters
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Occurrence and general properties of antibiotic transporters |
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Modulation of the absorption and elimination of antibiotics |
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Barrier effects |
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Modulation of cellular accumulation of antibiotics |
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Strategies for the future |
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Acknowledgements |
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