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Mini-Reviews in Medicinal Chemistry


ISSN (Print): 1389-5575
ISSN (Online): 1875-5607

Inhibitors of Multidrug Efflux Transporters: Their Membrane and Protein Interactions

Author(s): A. Seelig and E. Gatlik-Landwojtowicz

Volume 5, Issue 2, 2005

Page: [135 - 151] Pages: 17

DOI: 10.2174/1389557053402693

Price: $65


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

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