Modulation of the function of human MDR1 P-glycoprotein by the antimalarial drug mefloquine.

@article{Riffkin1996ModulationOT,
  title={Modulation of the function of human MDR1 P-glycoprotein by the antimalarial drug mefloquine.},
  author={Christopher D. Riffkin and Raymond Jia Jun Chung and Dominic M. Wall and John R Zalcberg and Alan F Cowman and Meredith Anne Foley and Leann Tilley},
  journal={Biochemical pharmacology},
  year={1996},
  volume={52 10},
  pages={
          1545-52
        }
}
MDR1 P-glycoprotein in membranes of human tumor cells of the CEM/VBL100 line was selectively labelled using photoreactive analogs of verapamil, N-(p-azido-3-[125I]salicyl)amino-verapamil ([125I]ASA-V) and prazosin, 2-[4-(4-azido-3-[125I]iodobenzoyl)piperazin-1-yl]4 -amino-6,7-dimethoxyyquinazoline ([125I]ASA-P). Mefloquine, a quinolinemethanol antimalarial drug, was shown to inhibit the labelling of P-glycoprotein with an efficiency similar to that for verapamil, a known chemosensitizer. By… CONTINUE READING
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