The key to unlocking the chemotherapeutic potential of PPAR ligands: Having the right combination

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Despite extensive preclinical evidence that peroxisome proliferator- activated receptor (PPAR) activation protects against tumourigenesis, results from a few clinical trials using PPAR ligands as monotherapy show modest success. In spite of this, several groups reported exciting results with therapeutic regimens that combine PPAR ligands with other compounds: chemotherapeutic agents, retinoid x receptor (RXR) agonists, statins, or cell-to-cell signaling molecules in preclinical cancer models and human trials. Here we have compiled an extensive review, consolidating the existing literature, which overwhelmingly supports a beneficial effect of treating with PPAR ligands in combination with existing chemotherapies versus their monotherapy in cancer. There are many examples in which combination therapy resulted in synergistic/additive effects on apoptosis, differentiation, and the ability to reduce cell growth and tumour burden. There are also studies that indicate that PPARγ ligand pretreatment overcomes resistance and reduces toxicities. Several mechanisms are explored to explain these protective effects. This paper highlights each of these studies that, collectively, make a very strong case for the use of PPAR ligands in combination with other agents in the treatment and management of several cancers. Copyright © 2012 Graham Skelhorne-Gross and Christopher J. B. Nicol.




Skelhorne-Gross, G., & Nicol, C. J. B. (2012). The key to unlocking the chemotherapeutic potential of PPAR ligands: Having the right combination. PPAR Research.

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