Interactions of the multidrug resistance modulators tariquidar and elacridar and their analogues with P-glycoprotein.

@article{Pajeva2013InteractionsOT,
  title={Interactions of the multidrug resistance modulators tariquidar and elacridar and their analogues with P-glycoprotein.},
  author={Ilza Pajeva and Katja Sterz and Matthias Christlieb and Kerstin Steggemann and Federico Marighetti and Michael Wiese},
  journal={ChemMedChem},
  year={2013},
  volume={8 10},
  pages={1701-13}
}
Tariquidar and elacridar are among the most potent inhibitors of the multidrug resistance transporter P-glycoprotein (P-gp), but how they interact with the protein is yet unknown. In this work, we describe a possible way in which these inhibitors interact with P-gp. We rely on structure-activity relationship analysis of a small group of tariquidar and elacridar analogues that was purposefully selected, designed, and tested. Structural modifications of the compounds relate to the presence or… CONTINUE READING