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PPAR Research
Volume 2012, Article ID 504918, 16 pages
Review Article

PPAR Medicines and Human Disease: The ABCs of It All

1Department of Pathology and Molecular Medicine, Queen's University, Kingston, ON, Canada K7L 3N6
2Cancer Biology and Genetics Division, Cancer Research Institute, Queen's University, Kingston, ON, Canada K7L 3N6
3Department of Biomedical and Molecular Sciences, Queen's University, Kingston, ON, Canada K7L 3N6

Received 24 February 2012; Revised 4 April 2012; Accepted 6 April 2012

Academic Editor: Yuji Kamijo

Copyright © 2012 Anthony J. Apostoli and Christopher J. B. Nicol. 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.


ATP-dependent binding cassette (ABC) transporters are a family of transmembrane proteins that pump a variety of hydrophobic compounds across cellular and subcellular barriers and are implicated in human diseases such as cancer and atherosclerosis. Inhibition of ABC transporter activity showed promise in early preclinical studies; however, the outcomes in clinical trials with these agents have not been as encouraging. Peroxisome proliferator-activated receptors (PPARs) are ligand-activated transcription factors that regulate genes involved in fat and glucose metabolism, and inflammation. Activation of PPAR signaling is also reported to regulate ABC gene expression. This suggests the potential of PPAR medicines as a novel means of controlling ABC transporter activity at the transcriptional level. This paper summarizes the advances made in understanding how PPAR medicines affect ABC transporters, and the potential implications for impacting on human diseases, in particular with respect to cancer and atherosclerosis.