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While MATE transporters are the final step in organic cation secretion in renal tubules and hepatocytes, most studies evaluating MATE activity and function have been performed in overexpressing cells that operate in an “uptake mode.” This is accomplished by creating a proton gradient that favors MATE uptake of organic cations from the external face of the plasma membrane. Evaluation of MATE transport in an uptake mode overcomes limitations with quantifying efflux from cells that may not be otherwise permeable to organic cation entry. The energetics and kinetics of transport by MATEs are considered similar while operating in either the uptake or efflux mode [25].

FIGURE 3.2 Examples of MATE inhibitors. Structures of chemical inhibitors were downloaded from public database. https://www.ebi.ac.uk/chebi/init.do.