Peroxisome proliferator-activated receptor alpha (PPAR alpha)
PPAR alpha is a nuclear receptor that plays a crucial role in the regulation of lipid and glucose metabolism, inflammation, and oxidative stress. It is primarily expressed in the liver but also in other metabolic tissues such as the skeletal muscle and heart. PPAR alpha is activated by endogenous fatty acids, as well as synthetic ligands such as fibric acid derivatives, which are used in the treatment of dyslipidemia. PPAR alpha activation leads to the upregulation of genes involved in fatty acid oxidation, resulting in a reduction in circulating triglycerides and an increase in high-density lipoprotein (HDL) cholesterol. In addition, PPAR alpha activation also has anti-inflammatory and antioxidant effects. Several drugs that target PPAR alpha, such as fibrates, are currently in clinical use for the treatment of dyslipidemia.
Peroxisome proliferator-activated receptor beta/delta (PPAR beta/delta)
PPAR beta/delta is a nuclear receptor that is involved in the regulation of lipid metabolism, glucose homeostasis, and inflammation. It is expressed in various tissues, including adipose tissue, skeletal muscle, and the liver. PPAR beta/delta is activated by endogenous fatty acids, as well as synthetic ligands such as GW501516, which has been shown to improve endurance performance in animal models. PPAR beta/delta activation leads to an increase in fatty acid oxidation and a decrease in lipogenesis, resulting in an improvement in insulin sensitivity and a reduction in circulating triglycerides. PPAR beta/delta is also involved in the regulation of inflammation and is a potential target for the treatment of inflammatory diseases such as atherosclerosis and inflammatory bowel disease. Several drugs that target PPAR delta, such as GW501516, are currently in various stages of preclinical and clinical development.