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Diabetes and Obesity: Peroxisome Proliferator - Activated Receptors (PPARs)
 
 
Peroxisome proliferator-activated receptors (PPARs) are members of the nuclear hormone receptor family of transcription factors that mediate a variety of cellular processes, including glucose and lipid metabolism, inflammatory responses, and regulation of apoptotic cell death. PPARg is shown to mediate the antidiabetic and adipogenic actions of the thiazolidinediones (TZDs), a new class of insulin sensitizers, which are under clinical trials for the treatment of Type II diabetes. TZDs are highly selective, high-affinity ligands of PPARg with minimal activity towards the a and b forms. Although PPARg is expressed in most organs, the level of PPARg mRNA is about 50-fold higher in the adipose tissue. In the cell, PPAR forms a heterodimer with the retinoid X receptor (RXR). When induced by TZDs, a conformational change occurs in the heterodimer and co-repressor complexes are displaced. This promotes binding of the PPAR-RXR complex to specific DNA sequences, PPRE, located in the regulatory regions of target genes. PPREs are commonly found in genes involved in lipid metabolism and energy balance, including those encoding lipoprotein lipase, adipocyte fatty acid binding protein, fatty acyl-CoA synthase, glucokinase, and glucose transporter GLUT4.
 
 
 
 
 
 
 
 
PPAR Agonists
 
PPAR Antagonists
 
PPAR Receptors and Antibodies to Receptor Related Proteins