Inhibitors of multidrug efflux transporters: their membrane and protein interactions.
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 (H-bonding potential, dimensions, and pK(a) values) as well as the properties of the membrane.
Seelig
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Biophysical Chemistry, Biozentrum, University of Basel, Klingelbergstrasse, Switzerland. Anna.Seelig@unibas.ch
Gatlik-Landwojtowicz
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D000818:Animals; D001692:Biological Transport; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D006801:Humans; D007700:Kinetics; D049990:Membrane Transport Modulators; D026901:Membrane Transport Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D008566:Membranes / Q000378:metabolism; D004364:Pharmaceutical Preparations / Q000378:metabolism*; D011506:Proteins / Q000037:antagonists & inhibitors / Q000378:metabolism; D013816:Thermodynamics
D049990:Membrane Transport Modulators; D026901:Membrane Transport Proteins; D004364:Pharmaceutical Preparations; D011506:Proteins