The progress and development of GLUT1 inhibitors targeting cancer energy metabolism

Abstract

A major difference between glucose metabolism in cancer cells and normal cells is that glucose in cancer cells is preferably converted to lactate in aerobic conditions rather than oxidized in mitochondria. This process is called aerobic glycolysis, known as the ‘Warburg effect’. In this review, we focus on the energy-metabolism characteristics between tumor and normal cells, analyzing the regulation mechanism of energy metabolism based on glycolysis, and summarizing two targets on the upstream proteins of glycolysis, including glucose transporter (GLUT) and hexokinase. In addition, we proposed the risks and limitations of GLUT1-based drug research and summarized the current research progress of representative drugs, including natural and synthetic GLUT1 inhibitors. This will provide guidance for designing and synthesizing small molecule drugs targeting GLUT1 in glycolysis.