Double-transfected MDCK cells expressing human OCT1/MATE1 or OCT2/MATE1: determinants of uptake and transcellular translocation of organic cations.

ABSTRACT:

Background and purpose

The organic cation transporters 1 (OCT1) and 2 (OCT2) mediate drug uptake into hepatocytes and renal proximal tubular cells, respectively. Multidrug and toxin extrusion protein 1 (MATE1) is a major component of subsequent export into bile and urine. However, the functional interaction of OCTs and MATE1 for uptake and transcellular transport of the oral antidiabetic drug metformin or of the cation 1-methyl-4-phenylpyridinium (MPP(+)) has not fully been characterized.

Experimental approach

Single-transfected Madin-Darby canine kidney (MDCK) cells as well as double-transfected MDCK-OCT1-MATE1 and -OCT2-MATE1 cells were used to study metformin and MPP(+) uptake into and transcellular transport across cell monolayers, along with their concentration and pH d

SUBMITTER: Konig J 

PROVIDER: S-EPMC3101617 | biostudies-literature | 2011 Jun

REPOSITORIES: biostudies-literature