Phase I and II metabolism and MRP2-mediated export of bosentan in a MDCKII-OATP1B1-CYP3A4-UGT1A1-MRP2 quadruple-transfected cell line.

Background And Purpose: Hepatic uptake (e.g. by OATP1B1), phase I and II metabolism (e.

Identification of drugs and drug metabolites as substrates of multidrug resistance protein 2 (MRP2) using triple-transfected MDCK-OATP1B1-UGT1A1-MRP2 cells.

Background And Purpose: The coordinate activity of hepatic uptake transporters [e.g. organic anion transporting polypeptide 1B1 (OATP1B1)], drug-metabolizing enzymes [e.

Functional and structural relevance of conserved positively charged lysine residues in organic anion transporting polypeptide 1B3.

The human organic anion transporting polypeptide 1B3 (OATP1B3), located in the basolateral membrane of hepatocytes, mediates the uptake of endogenous substrates such as taurocholate and drugs from blood into hepatocytes. The transport activity of OATP1B3 is influenced by positively charged amino acids, which are facing the central pore. Molecular modeling was performed to select conserved positively charged amino acids, which may influence transport activity and anchoring of OATP1B3 in the plasma membrane.

Hepatic OATP and OCT uptake transporters: their role for drug-drug interactions and pharmacogenetic aspects.

Uptake transporters in the basolateral membrane of hepatocytes are important for the hepatobiliary elimination of drugs. Further, since drug-metabolizing enzymes are located intracellularly, uptake into hepatocytes is a prerequisite for their subsequent metabolism. Therefore, alteration of uptake transporter function (e.