PPARbeta/delta ligands as modulators of the inflammatory response

Peroxisome proliferator-activated receptors (PPARs) are steroid hormone nuclear receptors encoded by three genes: alpha, gamma and beta/delta. Small-molecule agonists of this family of receptors, mostly PPARalpha and PPARgamma agonists, possess pronounced anti-inflammatory effects; however, the use of selective PPARbeta/delta agonists in preclinical studies suggests that this subtype also possesses anti-inflammatory properties. In vivo data suggest that ligands to the beta/delta isoform have activity in a number of disease models that are partly driven by the inflammatory response. Thus, selective activation of PPARbeta/delta may represent a promising therapeutic approach for the treatment of diseases that have inflammation as a central component of their pathophysiology. An overview of preclinical data that support the ability of PPARbeta/delta agonists to modulate the inflammatory response is provided.