2. Academic Validation
  3. Inhibitors of multidrug efflux transporters: their membrane and protein interactions

Inhibitors of multidrug efflux transporters: their membrane and protein interactions

  • Mini Rev Med Chem. 2005 Feb;5(2):135-51. doi: 10.2174/1389557053402693.
A Seelig 1,  E Gatlik-Landwojtowicz
Affiliations

Affiliation

  • 1 Biophysical Chemistry, Biozentrum, University of Basel, Klingelbergstrasse, Switzerland. [email protected]
PMID: 15720284 DOI: 10.2174/1389557053402693
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 (H-bonding potential, dimensions, and pK(a) values) as well as the properties of the membrane.

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