Molecular features, regulation, and function of monocarboxylate transporters: Implications for drug delivery

Bradley E. Enerson, Lester R. Drewes

Research output: Contribution to journalShort surveypeer-review

170 Scopus citations


The diffusion of monocarboxylates such as lactate and pyruvate across the plasma membrane of mammalian cells is facilitated by a family of integral membrane transport proteins, the monocarboxylate transporters (MCTs). Currently, at least eight unique members of the MCT family have been discovered and orthologs to each have been identified in a variety of species. Four MCTs (MCT1-MCT4) have been functionally characterized. Each isoform possesses unique biochemical properties such as kinetic constants and sensitivity to known MCT inhibitors. Several fold changes in the expression of MCTs may be evoked by altered physiological conditions, yet the molecular mechanisms underlying the regulation of MCTs are poorly understood. Post-translational regulation of MCT1 and MCT4 occurs, in part, by interaction with CD147, an accessory protein that is necessary for trafficking, localization, and functional expression of these transporters. Because of the physiological importance of monocarboxylates to the overall maintenance of metabolic homeostasis, the function of MCTs is significant to several pathologies that occur with disease, such as ischemic stroke and cancer. Finally, the expression of MCT1 in the epithelium of the small intestine and colon and in the blood-brain barrier may provide routes for the intestinal and blood to brain transfer of carboxylated pharmaceutical agents and other exogenous monocarboxylates.

Original languageEnglish (US)
Pages (from-to)1531-1544
Number of pages14
JournalJournal of Pharmaceutical Sciences
Issue number8
StatePublished - Aug 1 2003


  • Blood-brain barrier
  • Epithelium
  • Lactate
  • Monocarboxylate
  • Transport


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