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The organic anion transporting polypeptides (OATP/SLCO) belong to the solute carrier (SLC) transporter superfamily and primarily mediate cellular uptake of anionic substrates in diverse tissues, including the liver, small intestines, kidneys and blood–brain barrier. This chapter summarizes current knowledge about the function of OATP transporters, their preclinical characterization, and the structural determinants of OATP-mediated drug transport and drug–drug interactions with a focus on the liver-specific transporters OATP1B1 and OATP1B3.

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