Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.

@article{Schwab2003ComparisonOI,
  title={Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.},
  author={Dietmar Schwab and Holger Fischer and Azam Tabatabaei and Sonia Maria Poli and Joerg Huwyler},
  journal={Journal of medicinal chemistry},
  year={2003},
  volume={46 9},
  pages={
          1716-25
        }
}
The ATP-dependent drug efflux pump P-glycoprotein (P-gp) affects the absorption and disposition of many compounds. P-gp may also play role in clinically significant drug-drug interactions. Therefore, it is important to find potential substrates or inhibitors of P-gp early in the drug discovery process. To identify compounds that interact with this transporter, several P-gp assays were validated and compared by testing a set of 28 reference compounds, including inhibitors of cytochrome P450 3A4… CONTINUE READING
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