Multidrug and toxin extrusion protein 1 and 2-K (hMATE1/2-K)

The human multidrug and toxin extrusion transporters, hMATE1 (SLC47A1) and hMATE2-K (SLC47A2), are essential membrane proteins that facilitate the final step in the renal and hepatic excretion of organic cations [1, 5, 17]. These transporters function as H+/organic cation antiporters, utilizing an oppositely directed proton gradient to drive the efflux of various drugs and endogenous toxins into the urine and bile [4, 10, 18]. MATE1 is widely expressed in the liver, kidney, and other tissues, while MATE2-K is primarily localized to the brush-border membrane of the renal proximal tubule [5, 9, 17]. They play a critical role in the pharmacokinetics of widely used drugs such as the antidiabetic agent metformin and platinum-based chemotherapeutics like cisplatin [6, 10, 19]. Inhibition of these transporters by other drugs can lead to significant drug-drug interactions, increased systemic exposure, and potential nephrotoxicity due to the intracellular accumulation of toxic substrates [6, 11, 20]. Consequently, hMATE1 and hMATE2-K are key targets for evaluating drug safety and efficacy during pharmaceutical development [9, 16, 22].

Other names

SLC47A1 [5, 17]SLC47A2 [5, 17]MATE1 [1, 17]MATE2-K [1, 17]H+/organic cation antiporter [4, 18]Solute carrier family 47 member 1 [17]Solute carrier family 47 member 2 [17]

H+/organic cation antiporter that exchanges organic cations for protons to facilitate cellular efflux [1, 4, 10, 18].