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STF-31 is an experimental small molecule that acts as a dual inhibitor of glucose transporter 1 (GLUT1) and nicotinamide phosphoribosyltransferase (NAMPT). It was originally identified for its selective cytotoxicity against renal cell carcinoma (RCC) cells lacking the von Hippel-Lindau (VHL) tumor suppressor gene, exploiting their dependence on GLUT1-mediated glucose uptake and aerobic glycolysis. By inhibiting GLUT1, STF-31 impedes glucose transport into cancer cells, disrupting energy metabolism—a phenomenon known as the Warburg effect. Additionally, it inhibits NAMPT, a key enzyme in NAD+ biosynthesis critical for cellular metabolism and survival. The compound has demonstrated antineoplastic activity in preclinical models but is not approved for clinical use. Its efficacy appears to depend on the expression levels of GLUT1 and NAMPT in target tumors[2][4][5][6][8].
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