Peroxisome proliferator-activated receptors (PPARs) are ligand-activated transcription factors belonging to a nuclear hormone receptor superfamily, containing three isoforms (α, β/δ, and γ). PPARs are activated by naturally occurring fatty acids or fatty acid derivatives (e.g. eicosanoids) and play a critical physiological role in the regulation of numerous biological processes, including lipid and glucose metabolism, and overall energy homeostasis. Clinically, PPAR ligands like Glitazones (also known as Thiazolidinediones (TDZs)) are used for treatment of type 2 diabetes by decreasing insulin resistance. In addition, PPARs also have been implicated as modulators of obesity-induced inflammation making them interesting therapeutic targets to mitigate obesity-induced inflammation and its consequences. Heterodimers of PPAR and Retinoid X Receptor (RXR) form important transcription activators which upon binding PPAR response elements (PPRE) can modulate many important cell functions. For example, PPARα-RXR dimers activate target genes which control peroxisome proliferation, fatty acid metabolism and lipid homeostasis, while PPARγ-RXR dimers affect adipocyte differentiation, glucose and insulin homeostasis and macrophage function.