Recent Progress in the Development of Glucose Transporter (GLUT) Inhibitors

Cancer cells exhibit an accelerated glucose uptake and glycolysis. The transmembrane uptake of glucose requires specific carrier proteins, such as glucose transporters (GLUTs) and sodium-coupled glucose cotransporters (SGLTs). GLUTs transport glucose independently of the energy supply and have become promising targets for cancer therapy. This Perspective mainly focuses on the current research progress and design strategy of GLUT inhibitors, particularly those targeting class I (GLUT1–4). To the best of our knowledge, this is the first systematic interpretation of the research progress, opportunities, and challenges faced in the development of GLUT inhibitors from a medicinal chemistry perspective. We hope that this Perspective will provide insights into the development of GLUT inhibitors, offering a feasible approach to cancer therapy.