Enantioselective activation of the peroxisome proliferator-activated receptor.

Enantioselective activation of the peroxisome proliferator-activated receptor.

A cell-based transactivation assay was established using the mouse full-length peroxisome proliferator-activated receptor (PPAR) cDNA sequence and the positive peroxisome proliferator-responsive regulatory element (-578 to -553) of the rat acyl-CoA oxidase gene promoter. Activation of the reporter plasmid was dependent on co-transfection of the full-length PPAR cDNA, and the response was greatl...

Peroxisome Proliferator-Activated Receptor

Peroxisome proliferator - activated receptor

The peroxisome proliferator-activated receptors (PPARs) belong to the nuclear hormone receptor superfamily. All PPARs heterodimerize with the retinoid X receptor (RXR) and bind to specific regions on the DNA of target genes. The discovery of PPARγ as a target of multimodal insulin sensitizers has attracted remarkable scientific interest and had a great impact on the pharmaceutical industry. Thi...

Peroxisome Proliferator-Activated Receptor

Mode of peroxisome proliferator-activated receptor γ activation by luteolin.

The peroxisome proliferator-activated receptor γ (PPARγ) is a target for treatment of type II diabetes and other conditions. PPARγ full agonists, such as thiazolidinediones (TZDs), are effective insulin sensitizers and anti-inflammatory agents, but their use is limited by adverse side effects. Luteolin is a flavonoid with anti-inflammatory actions that binds PPARγ but, unlike TZDs, does not pro...