The P-Glycoprotein Efflux Pump: How Does it Transport Drugs?

The P-Glycoprotein Efflux Pump: How Does it Transport Drugs? J. Membrane Biol. 160, 161–175 (1997) The Journal of Membrane Biology © Springer-Verlag New York Inc. 1997 Topical Review F.J. Sharom Guelph-Waterloo Centre for Graduate Work in Chemistry and Biochemistry, University of Guelph, Guelph, Ontario Canada N1G 2W1 Received: 3 April 1997/Revised: 11 June 1997 Introduction drug-resistant tumors [29–32], and many Phase I and II clinical trials have been carried out, or are in progress. The development of multidrug resistance (MDR) is a Pgp is also found in several normal human tissues, in- major obstacle in the chemotherapeutic treatment of cluding the apical surface of many epithelial cells and the many human cancers, including colon, kidney and breast endothelial cells of the blood brain barrier. Its physi- carcinomas, leukemias, multiple myeloma, and pediatric ological role is not yet clear, although it appears to be cancers. Resistant tumors are found to be cross-resistant involved in protection against toxic natural products. to a broad but well-defined spectrum of structurally un- This review will focus on the molecular properties of related cytotoxic drugs, including the Vinca alkaloids, Pgp with respect to binding and transport of substrates, anthracyclines, epipodophyllotoxins, and taxanes (Table and how these properties can be related to the possible 1). The Journal of Membrane Biology Springer Journals

The P-Glycoprotein Efflux Pump: How Does it Transport Drugs?

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Copyright © Inc. by 1997 Springer-Verlag New York
Life Sciences; Biochemistry, general; Human Physiology
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