2021•Royal Society of Chemistry eBooksRequires access

OATPs: The SLCO Family of Organic Anion Transporting Polypeptide Transporters

Maria Karlgren, Pär Matsson

Abstract

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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Available abstract

Key concepts: Transporter, Organic anion-transporting polypeptide, Organic anion transporter 1, Solute carrier family, Drug, Chemistry, Pharmacology, Biochemistry