| Summary: | In this review, the history of the peroxisome proliferator-activated receptors (PPARα, PPARβ/δ and PPARγ) discovery is briefly traced and major features of their structure and posttranslational modifications are presented. Furthermore, an overview of PPAR coactivators and corepressors as well as of endogenous and exogenous ligands is discussed. We have also summarized significant efforts underway to develop more effective and safer PPAR modulators as therapeutic agents to treat diseases such as diabetes, cancer, atherosclerosis, and inflammation. Finally, we share a hypothesis proposing how PPARs may control inflammatory events.
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