Inhibitors of Multidrug Efflux Transporters: Their Membrane and Protein Interactions

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.

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