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Colin A Flaveny, Kristine Griffett, Bahaa El-Dien M El-Gendy, Melissa Kazantzis, Monideepa Sengupta, Antonio L Amelio, Arindam Chatterjee, John Walker, Laura A Solt, Theodore M Kamenecka, Thomas P Burris
Malignant cells exhibit aerobic glycolysis (the Warburg effect) and become dependent on de novo lipogenesis, which sustains rapid proliferation and resistance to cellular stress. The nuclear receptor liver-X-receptor (LXR) directly regulates expression of key glycolytic and lipogenic genes. To disrupt these oncogenic metabolism pathways, we designed an LXR inverse agonist SR9243 that induces LXR-corepressor interaction. In cancer cells, SR9243 significantly inhibited the Warburg effect and lipogenesis by reducing glycolytic and lipogenic gene expression...
July 13, 2015: Cancer Cell
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