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:
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
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