Anthony M. Barsotti

To further investigate the synergy between GLUT inhibition and complex I blockade, we determined KL-11743 cell proliferation IC50 values alone and in combination with the complex I inhibitors phenformin, pyrvinium pamoate, and rotenone. Complex I inhibitors, at doses that do not inhibit proliferation as single agents, decreased the IC50 of KL-11743 by approximately 3-fold (Figures S3C and S3D).

Aerobic glycolysis, originally identified by Warburg as a hallmark of cancer, has recently been implicated in immune cell activation and growth. Glucose, the starting material for glycolysis, is transported through the cellular membrane by a family of glucose transporters (GLUTs). Therefore, targeting glucose transporters to regulate aerobic glycolysis is an attractive approach to identify potential therapeutic agents for cancers and autoimmune diseases.