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ChemMedChem. 2018 Feb 6;13(3):209-219. doi: 10.1002/cmdc.201700703. Epub 2018 Jan 10.

The Anticancer Potential of Peroxisome Proliferator-Activated Receptor Antagonists.

Author information

1
Department of Pharmacy, University of Chieti, Via dei Vestini 31, 66100, Chieti, Italy.
2
Unit of General Pathology, CeSI-MeT, University of Chieti, Chieti, Italy.
3
Department of Life, Health and Environmental Sciences, University of L'Aquila, L'Aquila, Italy.
4
National Institute for Nuclear Physics (INFN), Gran Sasso National Laboratory (LNGS), Assergi (Aq), Italy.
5
Sbarro Institute for Cancer Research and Molecular Medicine and Center for Biotechnology, Temple University, 1900 N. 12th Street, Philadelphia, PA, 19122, USA.

Abstract

The effects on cancer-cell proliferation and differentiation mediated by peroxisome proliferator-activated receptors (PPARs) have been widely studied, and pleiotropic outcomes in different cancer models and under different experimental conditions have been obtained. Interestingly, few studies report and little preclinical evidence supports the potential antitumor activity of PPAR antagonists. This review focuses on recent findings on the antitumor in vitro and in vivo effects observed for compounds able to inhibit the three PPAR subtypes in different tumor models, providing a rationale for the use of PPAR antagonists in the treatment of tumors expressing the corresponding receptors.

KEYWORDS:

PPAR antagonists; antitumor agents; cytotoxicity; metabolic drugs; nuclear receptors

PMID:
29276815
DOI:
10.1002/cmdc.201700703

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