Multidrug and toxin extrusion protein 1 (MATE1) (hMATE1)

Human multidrug and toxin extrusion protein 1 (hMATE1), encoded by the SLC47A1 gene, is a critical H+/organic cation antiporter primarily localized to the apical membrane of renal proximal tubule cells and the canalicular membrane of hepatocytes. It serves as a multidrug efflux pump, facilitating the final step in the excretion of a broad range of cationic drugs and endogenous metabolites into urine and bile. Key substrates include the widely used antidiabetic drug metformin, the chemotherapeutic agent oxaliplatin, and the endogenous biomarker creatinine. Due to its central role in drug disposition, hMATE1 is a major site for clinically significant drug-drug interactions, where its inhibition can lead to elevated systemic drug levels and increased risk of toxicity. Additionally, hMATE1 expression is often dysregulated in certain cancers, such as glioblastoma, where it may contribute to chemoresistance and tumor progression. Understanding the functional and genetic landscape of hMATE1 is vital for predicting drug clearance and optimizing personalized medicine strategies.

Other names

SLC47A1Solute carrier family 47 member 1MATE1Multidrug and toxin extrusion protein 1

Functions as an H+/organic cation antiporter that mediates the efflux of cationic drugs and endogenous metabolites from cells into the tubular lumen of the kidney or the bile canaliculi of the liver in exchange for protons.