Physiological and pharmacokinetic roles of H+/organic cation antiporters (MATE/SLC47A)

Biochem Pharmacol. 2008 May 1;75(9):1689-96. doi: 10.1016/j.bcp.2007.12.008. Epub 2007 Dec 27.


Vectorial secretion of cationic compounds across tubular epithelial cells is an important function of the kidney. This uni-directed transport is mediated by two cooperative functions, which are membrane potential-dependent organic cation transporters at the basolateral membranes and H+/organic cation antiporters at the brush-border membranes. More than 10 years ago, the basolateral organic cation transporters (OCT1-3/SLC22A1-3) were isolated, and molecular understandings for the basolateral entry of cationic drugs have been greatly advanced. However, the molecular nature of H+/organic cation antiport systems remains unclear. Recently, mammalian orthologues of the multidrug and toxin extrusion (MATE) family of bacteria have been isolated and clarified to function as H+/organic cation antiporters. In this commentary, the molecular characteristics and pharmacokinetic roles of mammalian MATEs are critically overviewed focusing on the renal secretion of cationic drugs.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Antiporters / genetics
  • Antiporters / metabolism
  • Antiporters / physiology*
  • Cell Membrane / metabolism
  • Cloning, Molecular
  • Humans
  • Hydrogen* / physiology
  • Kidney / metabolism
  • Molecular Sequence Data
  • Organ Specificity
  • Organic Cation Transport Proteins / genetics
  • Organic Cation Transport Proteins / metabolism
  • Organic Cation Transport Proteins / physiology*
  • Pharmaceutical Preparations / metabolism*
  • Pharmaceutical Preparations / urine
  • Substrate Specificity
  • Xenobiotics / pharmacokinetics*
  • Xenobiotics / urine


  • Antiporters
  • Organic Cation Transport Proteins
  • Pharmaceutical Preparations
  • Xenobiotics
  • Hydrogen