Abstract
Modulators and inhibitors of multidrug efflux transporters, like P-glycoprotein, are used to reduce or inhibit multidrug resistance, MDR, which leads to a failure of the chemotherapy of e.g. cancers, epilepsy, bacterial, parasitic, and fungal diseases. Binding and transport of first-, second-, and third-generation modulators and inhibitors of P-glycoprotein are discussed, taking into account the properties of the drug (Hbonding potential, dimensions, and pKα values) as well as the properties of the membrane.
Keywords: p-glycoprotein, first, second, and third-generation inhibitors, modulators, membrane partitioning, transporter binding, transport kinetics
Mini-Reviews in Medicinal Chemistry
Title: Inhibitors of Multidrug Efflux Transporters: Their Membrane and Protein Interactions
Volume: 5 Issue: 2
Author(s): A. Seelig and E. Gatlik-Landwojtowicz
Affiliation:
Keywords: p-glycoprotein, first, second, and third-generation inhibitors, modulators, membrane partitioning, transporter binding, transport kinetics
Abstract: Modulators and inhibitors of multidrug efflux transporters, like P-glycoprotein, are used to reduce or inhibit multidrug resistance, MDR, which leads to a failure of the chemotherapy of e.g. cancers, epilepsy, bacterial, parasitic, and fungal diseases. Binding and transport of first-, second-, and third-generation modulators and inhibitors of P-glycoprotein are discussed, taking into account the properties of the drug (Hbonding potential, dimensions, and pKα values) as well as the properties of the membrane.
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Cite this article as:
Seelig A. and Gatlik-Landwojtowicz E., Inhibitors of Multidrug Efflux Transporters: Their Membrane and Protein Interactions, Mini-Reviews in Medicinal Chemistry 2005; 5 (2) . https://dx.doi.org/10.2174/1389557053402693
DOI https://dx.doi.org/10.2174/1389557053402693 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
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