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The SLC22 transporters belong to the solute carrier (SLC) transporter superfamily and have diverse functions and expression patterns that include the cellular uptake of organic cations, anions and zwitterions in the liver and kidneys. Important members from a pharmacokinetic perspective include the organic anion transporters 1–3 (OAT1–3) and the organic cation transporters 1 and 2 (OCT1 and OCT2). This chapter summarizes current knowledge about the function of OATs and OCTs, their preclinical characterization and the structural determinants of OAT- and OCT-mediated drug transport and drug–drug interactions.

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