Structure-Based Identification of OATP1B1/3 Inhibitors

@article{Bruyn2013StructureBasedIO,
  title={Structure-Based Identification of OATP1B1/3 Inhibitors},
  author={T. de Bruyn and G. V. van Westen and A. IJzerman and B. Stieger and P. D. de Witte and P. Augustijns and P. Annaert},
  journal={Molecular Pharmacology},
  year={2013},
  volume={83},
  pages={1257 - 1267}
}
Several recent studies show that inhibition of the hepatic transport proteins organic anion-transporting polypeptide 1B1 (OATP1B1) and 1B3 (OATP1B3) can result in clinically relevant drug-drug interactions (DDI. [...] Key Method A total of 2000 compounds were tested as potential modulators of the uptake of the OATP1B substrate sodium fluorescein, in OATP1B1- or 1B3-transfected Chinese hamster ovary cells. At an equimolar substrate-inhibitor concentration of 10 µM, 212 and 139 molecules were identified as…Expand
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