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ChemMedChem. 2013 Oct;8(10):1609-16. doi: 10.1002/cmdc.201300250. Epub 2013 Aug 12.

Blocking the peroxisome proliferator-activated receptor (PPAR): an overview.

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Dipartimento di Farmacia, Università "G. d'Annunzio" via dei Vestini 31, 66100 Chieti (Italy).


Peroxisome proliferator-activated receptors (PPARs) have been studied extensively over the last few decades and have been assessed as molecular targets for the development of drugs against metabolic disorders. A rapid increase in understanding of the physiology and pharmacology of these receptors has occurred, together with the identification of novel chemical structures that are able to activate the various PPAR subtypes. More recent evidence suggests that moderate activation of these receptors could be favorable in pathological situations due to a decrease in the side effects brought about by PPAR agonists. PPAR partial agonists and antagonists are interesting tools that are currently used to better elucidate the biological processes modulated by this family of nuclear receptors. Herein we present an overview of the various molecular structures that are able to block each of the PPAR subtypes, with a focus on promising therapeutic applications.


PPARs; antagonists; isoform selectivity; receptors; structure–activity relationships

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