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Broad Anti-tumor Activity of a Small Molecule That Selectively Targets the Warburg Effect and Lipogenesis

Broad Anti-tumor Activity of a Small Molecule That Selectively Targets the Warburg Effect and Lipogenesis

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

Cancer Cell. 2015 Jul 13;28(1):42-56.

PMID: 26120082

Abstract:

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. SR9243 induced apoptosis in tumors without inducing weight loss, hepatotoxicity, or inflammation. Our results suggest that LXR inverse agonists may be an effective cancer treatment approach.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP1613028811	SR9243		1613028-81-1	Price

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