Identification of residues in the drug translocation pathway of the human multidrug resistance P-glycoprotein by arginine mutagenesis.

@article{Loo2009IdentificationOR,
  title={Identification of residues in the drug translocation pathway of the human multidrug resistance P-glycoprotein by arginine mutagenesis.},
  author={T. Y. Wings Loo and M. Claire Bartlett and David R. Clarke},
  journal={The Journal of biological chemistry},
  year={2009},
  volume={284 36},
  pages={
          24074-87
        }
}
P-glycoprotein (P-gp, ATP-binding cassette B1) is a drug pump that extracts toxic drug substrates from the plasma membrane and catalyzes their ATP-dependent efflux. To map the residues in the drug translocation pathway, we performed arginine-scanning mutagenesis on all transmembrane (TM) segments (total = 237 residues) of a P-gp processing mutant (G251V) defective in folding (15% maturation efficiency) (glycosylation state used to monitor folding). The rationale was that arginines introduced… CONTINUE READING
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Mapping the Drug Translocation Pathway of P-gp

T. W. Loo, D. M. Clarke
Expert Rev. Mol. Med • 2007