Background: Monocarboxylate Transporter 1 (MCT1), an important membrane transport protein, mediates
the translocation of monocarboxylates together with protons across biological membranes. Due to its pathological
significance, MCT1 plays an important role in the progression of some diseases, such as brain diseases and cancers.
Methods: We summarize the general description of MCT1 and provide a comprehensive understanding of the role of
MCT1 in brain diseases and cancers. Furthermore, this review discusses the opportunities and challenges of MCT1-
targeting drug-delivery systems in the treatment of brain diseases and cancers.
Results: In the brain, loss of MCT1 function is associated with pathologies of degeneration and injury of the nervous
system. In tumors, MCT1 regulates the activity of signaling pathways and controls the exchange of monocarboxylates
in aerobic glycolysis to affect tumor metabolism, proliferation and invasion. Meanwhile, MCT1 also acts as a
good biomarker for the prediction and diagnosis of cancer progressions.
Conclusion: MCT1 is an attractive transporter in brain diseases and cancers. Moreover, the development of MCT1-
based small molecule drugs and MCT1 inhibitors in the clinic is promising. This review systematically summarizes
the basic characteristics of MCT1 and its role in brain diseases and cancers, laying the foundation for further research