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Oncol Lett. 2018 Apr;15(4):4358-4364. doi: 10.3892/ol.2018.7843. Epub 2018 Jan 23.

LY294002 inhibits the Warburg effect in gastric cancer cells by downregulating pyruvate kinase M2.

Lu J1,2,3, Chen M1,3, Gao S3, Yuan J3, Zhu Z3, Zou X1,3.

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Department of Gastroenterology, The Affiliated Drum Tower Clinical Medical School of Nanjing Medical University, Nanjing, Jiangsu 210008, P.R. China.
Department of Gastroenterology, The Affiliated Wuxi Second Hospital of Nanjing Medical University, Wuxi, Jiangsu 214002, P.R. China.
Department of Gastroenterology, The Affiliated Drum Tower Hospital of Nanjing University, Medical School, Nanjing, Jiangsu 210008, P.R. China.


The 'Warburg effect' is considered a vital hallmark of cancer cells, characterized by an altered metabolism, in which cells rely on aerobic glycolysis. As a key enzyme of aerobic glycolysis, pyruvate kinase M2 (PKM2) serves a crucial role in tumorigenesis. Accumulating studies have indicated that PKM2 is a potential target for cancer therapy. The aim of the present study was to assess the anticancer effects of LY294002, a specific phosphatidylinositol-3-kinase inhibitor, on gastric cancer (GC) cells and further explore its possible mechanism in vitro. The present study revealed that LY294002 inhibited GC cell proliferation, induced early apoptosis and significantly decreased lactate dehydrogenase activity and lactate production, in part through inhibiting PKM2 expression. In summary, LY294002 exhibits anticancer effects on GC, partly via the downregulation of PKM2.


LY294002; Warburg effect; gastric cancer; glycolysis; pyruvate kinase M2

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