Transmembrane inhibitors of P-glycoprotein, an ABC transporter.

@article{Tarasova2005TransmembraneIO,
  title={Transmembrane inhibitors of P-glycoprotein, an ABC transporter.},
  author={Nadya I. Tarasova and Rishi Seth and Sergey G Tarasov and Teresa Kosakowska-Cholody and Christine A Hrycyna and Michael M. Gottesman and Christopher J. Michejda},
  journal={Journal of medicinal chemistry},
  year={2005},
  volume={48 11},
  pages={
          3768-75
        }
}
Drug resistance mediated by ABC transporters such as P-glycoprotein (P-gp) continues to be a major impediment to effective cancer chemotherapy. We have developed a panel of highly specific peptide inhibitors of P-gp based on the structure of the transmembrane domains of the transporter. These peptides are thought to exert their inhibitory action by disrupting the proper assembly of P-gp. A novel 96-well-plate assay based on the efflux of fluorescent P-gp substrate DiOC2 (3-ethyl-2-[3-(3-ethyl-2… CONTINUE READING
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