OATP - Organic Anion Transporting Polypeptide


OATP - Organic Anion Transporting Polypeptide


The members of the organic anion transporting polypeptide superfamily (OATPs, gene family: SLCO; former SLC21) are membrane transporters with 12 transmembrane domains that mediate sodium-independent the transport of a broad range of endo- and xenobiotics. Although most substrates are amphipathic organic anions with a molecular weight of more than 300 Da, some of the OATPs are transporters for neutral or positively charged substrates. Known substrates are, e.g., bile salts, triiodothyronine (T3), thyroxine (T4), prostaglandins, statins, antibiotics, anticancer agents and cardiac glycosides. Eleven OATPs are known in humans expressed in a variety of different human tissues including brain, intestine, liver and kidney and are involved in drug absorption, distribution, and excretion. Because of the wide tissue expression and broad substrate spectrum, OATPs can be determinates for alteration of drug kinetics.
Moreover, known genetic variants of OATPs are known to influence the transporter-mediated uptake of drugs resulting in a reduced or increased drug bioavailability with possible severe side effects and/or drug-drug interaction (DDI).


In cooperation with the University Medicine of Greifswald, Department of Clinical Pharmacology, Primacyt is offering a broad range of stable transfected HEK293 and MDCK2 cells expressing human OATPs. All cells are validated for expression rates, localization of the overexpressed transporter protein and functionality. We analyze the uptake functions using suitable substrates, inhibiting the uptake by adding the reference inhibitors.