Glycolysis-related enzymes and transporters

Glycolysis-related enzymes and transporters encompass a broad set of proteins that mediate the uptake and catabolism of glucose to generate ATP and biosynthetic precursors. Key components include the glucose transporter (GLUT) family, rate-limiting enzymes like Hexokinase 2 (HK2) and Pyruvate Kinase M2 (PKM2), and monocarboxylate transporters (MCTs) (Source: UniProt). In malignant cells, these proteins are often overexpressed to support the Warburg effect, a metabolic shift toward aerobic glycolysis that fuels rapid tumor growth and survival (Source: NIH). Pharmacological inhibition of these targets aims to selectively starve cancer cells or modulate metabolic disorders like diabetes. For instance, inhibitors of GLUT1 or HK2 can reduce the glucose flux, while MCT inhibitors prevent the export of lactate, leading to toxic intracellular accumulation (Source: PubMed). However, the essential role of glycolysis in normal physiology, especially in the central nervous system and erythrocytes, presents a major challenge for developing drugs with an acceptable therapeutic window (Source: PubMed). Safety concerns such as hypoglycemia and neurotoxicity must be carefully managed in clinical development (Source: Nature Reviews Drug Discovery). Despite these challenges, targeting the glycolytic machinery remains a promising area for metabolic reprogramming therapy in oncology and inflammatory diseases.

Other names

Glycolytic pathwayGlucose metabolism enzymesWarburg effect proteinsGlycolytic enzymes and transporters

Inhibition of glucose uptake via GLUT transporters, inhibition of rate-limiting enzymes such as Hexokinase or Phosphofructokinase to deplete ATP, or blockade of lactate export via MCT transporters to induce lethal intracellular acidosis (Source: PubMed).