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PFK15 is a small molecule inhibitor of 6-phosphofructo-2-kinase/fructose-2,6-biphosphatase 3 (PFKFB3), a key enzyme that regulates glycolytic flux in cancer cells by controlling the levels of fructose-2,6-bisphosphate. By inhibiting PFKFB3, PFK15 effectively blocks glycolysis, a metabolic pathway that is often upregulated in aggressive and chemoresistant tumors. Preclinical research, including studies presented at AACR 2024, has demonstrated that PFK15 can induce metabolic collapse and apoptosis in small cell lung cancer (SCLC) models. This effect is significantly enhanced when PFK15 is used in combination with other metabolic inhibitors, such as the MCT1 lactate transporter inhibitor SR13800, which targets adaptive metabolic circuits and provokes synthetic lethality in recalcitrant malignancies.
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