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PPAR Research
Volume 2012 (2012), Article ID 304760, 23 pages
Review Article

PPARs: Interference with Warburg’ Effect and Clinical Anticancer Trials

1Inserm, HMNO, CBP, CHRU Lille, 59037 Lille, France
2Biochemistry and Molecular Biology, HMNO, CBP, CHRU Lille, 59037 Lille, France
3Department of Human Biology and Toxicology, Faculty of Medicine and Pharmacy, UMons, 7000 Mons, Belgium
4Organic Chemistry Laboratory, Faculty of Sciences, UMons, 7000 Mons, Belgium
5Inserm U1065, IFR 50, Mediterranean Center of Molecular Medicine, 06204 Nice, France

Received 14 December 2011; Revised 15 February 2012; Accepted 19 February 2012

Academic Editor: Dipak Panigrahy

Copyright © 2012 Joseph Vamecq et al. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.


The metabolic/cell signaling basis of Warburg’s effect (“aerobic glycolysis”) and the general metabolic phenotype adopted by cancer cells are first reviewed. Several bypasses are adopted to provide a panoramic integrated view of tumoral metabolism, by attributing a central signaling role to hypoxia-induced factor (HIF-1) in the expression of aerobic glycolysis. The cancer metabolic phenotype also results from alterations of other routes involving ras, myc, p53, and Akt signaling and the propensity of cancer cells to develop signaling aberrances (notably aberrant surface receptor expression) which, when present, offer unique opportunities for therapeutic interventions. The rationale for various emerging strategies for cancer treatment is presented along with mechanisms by which PPAR ligands might interfere directly with tumoral metabolism and promote anticancer activity. Clinical trials using PPAR ligands are reviewed and followed by concluding remarks and perspectives for future studies. A therapeutic need to associate PPAR ligands with other anticancer agents is perhaps an important lesson to be learned from the results of the clinical trials conducted to date.