MATE2K (SLC47A2)
➦ Three major splice variants of the human multidrug and toxin extrusion transporter MATE2 have been identified, MATE2, MATE2-B and MATE2K. Human MATE2K consists of 566 amino acids and is mainly expressed in the kidney, where it is localized in the luminal membrane of proximal tubular epithelial cells.
| Main localization: | Kidney |
| Transporter assay: | Uptake transporter assay (potential substrate and inhibitor) |
| Probe substrates: | Metformin, 1-methyl-4-phenyl-pyridinium (MPP) |
| Probe inhibitors: | Cimetidine, ketoconazole |
| Regulatory relevance: | FDA guidance, EMA considered |
| Important interacting drugs: | Cimetidine, metformin, topotecan, cetirizine, procainamide, quinidine, ranitidine, verapamil, ketoconazole |
➦ Concentration dependent inhibition of hMATE2K-mediated metformin uptake by the probe inhibitor cimetidine
