Inhibition of Glucose Transporters and Glutaminase Synergistically Impairs Tumor Cell Growth (Cell Chemical Biology)

Cell-based screening identified the piperazin-2-one Glutor as a nanomolar inhibitor of glucose uptake that targets the glucose transporters GLUT-1/-3. Glutor inhibits glycolysis and effectively incudes cell death of monolayer- and spheroid-cultured cancer cells. Glutor-mediated glucose starvation upregulates GLUT-1/-3 expression. Glutor and glutaminase inhibitor CB-839 synergistically inhibit cancer cell growth.