Peroxisome proliferator-activated receptors (PPARs) were discovered in 1990 and belong to the steroid hormone receptors superfamily. Three PPAR subtypes have been discovered so far: PPARα, PPARβ/δ, and PPARγ. Human peroxisome proliferator-activated receptors (hPPARs) were initially identified as therapeutic targets for production of drugs to treat metabolic disorders, such as diabetes and dyslipidemia but now they are used in energy burning, dyslipidemia, diabetes, inflammation, hepatic steatosis, liver cancer, diabetic neuropathy, and atherosclerosis. These are included in the management of NIDDM, macrophage differentiation, adipose differentiation, anti-cancer processes, inhibition of TH2 cytokine production and rheumatoid arthritis. PPARβ/δ can be used to treat Huntington’s disease, fertility disorders, and dyslipidemia. The functions of third PPAR isoforms and their ability as a therapeutic target are still unknown.