Interaction of three regiospecific amino acid residues is required for OATP1B1 gain of OATP1B3 substrate specificity.

@article{DeGorter2012InteractionOT,
  title={Interaction of three regiospecific amino acid residues is required for OATP1B1 gain of OATP1B3 substrate specificity.},
  author={Marianne K. DeGorter and Richard Ho and Brenda F. Leake and Rommel G. Tirona and Richard B Kim},
  journal={Molecular pharmaceutics},
  year={2012},
  volume={9 4},
  pages={986-95}
}
The human organic anion-transporting polypeptides OATP1B1 (SLCO1B1) and OATP1B3 (SLCO1B3) are liver-enriched membrane transporters of major importance to hepatic uptake of numerous endogenous compounds, including bile acids, steroid conjugates, hormones, and drugs, including the 3-hydroxy-3-methylglutaryl Co-A reductase inhibitor (statin) family of cholesterol-lowering compounds. Despite their remarkable substrate overlap, there are notable exceptions: in particular, the gastrointestinal… CONTINUE READING
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