Linking Induction and Transrepression of PPARβ/δ with Cellular Function

Peroxisome proliferator activated receptors (PPARs) are ligand-activated transcription factors andmembers of the nuclear hormone receptor superfamily. PPARβ/δ is ubiquitously expressed andhas a central role in homeostasis, and has been suggested as a therapeutic target for a number ofmetabolic and cardiovascular disorders. This important nuclear receptor controls transcriptionunder different modes of molecular activity which directly control the cellular function and fate oftissues. This complex activity of induction and transrepression of gene expression (with and withoutexogenous ligands) is poorly understood and yet understanding this molecular control throughnovel drug development would led to control over a key molecular switch in all cells. This reviewoutlines the main molecular mechanisms of PPARβ/δ, and links the modes of activity to thesignalling pathways in inflammation, proliferation and senescence, with the goal to understand howthis will translate into novel drug design to control the PPARβ/δ molecular switch.