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Overview
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Background
PKM2 inhibitor (compound 3k) is a potent, selective inhibitor of pyruvate kinase M2 (PKM2) with the IC50 value of 2.95 μM. PKM2 is a rate-limiting enzyme of the glycolytic pathway which is preferentially expressed in various tumors. Cancer cells rely heavily on PKM2 for aerobic glycolysis, and specific targeting of PKM2 therefore offers a potential strategy for cancer therapy.
1. Ning X, Qi H, Li R, et al. Discovery of novel naphthoquinone derivatives as inhibitors of the tumor cell specific M2 isoform of pyruvate kinase. European Journal of Medicinal Chemistry, 2017, 138: 343-352.
2. Park JH, Kundu A, Lee SH, et al. Specific pyruvate kinase M2 inhibitor, compound 3k, induces autophagic cell death through disruption of the glycolysis pathway in ovarian cancer cells. International Journal of Biological Sciences, 2021, 17(8): 1895-1908.
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Overview