1932

Abstract

The nuclear peroxisome proliferator–activated receptor γ (PPARγ) is a transcription factor that is activated by polyunsaturated fatty acids and their metabolites and is essential for fat cell formation. Although obesity is a strong risk factor for type 2 diabetes mellitus and other metabolic diseases, potent PPARγ activators such as the glitazone drugs lower glucose and lipid levels in patients with type 2 diabetes and also have antiatherosclerotic and antihypertensive effects. We review recent studies providing insight into the paradoxical relationship between PPARγ and metabolic disease. We also review recent advances in understanding the structural basis for PPARγ activation by ligands. The unusual ligand-binding properties of PPARγ suggest that it will be possible to discover new chemical classes of receptor “modulators” with distinct pharmacological activities for the treatment of type 2 diabetes and other metabolic diseases.

Loading

Article metrics loading...

/content/journals/10.1146/annurev.biochem.70.1.341
2001-07-01
2024-04-15
Loading full text...

Full text loading...

/content/journals/10.1146/annurev.biochem.70.1.341
Loading
/content/journals/10.1146/annurev.biochem.70.1.341
Loading

Data & Media loading...

  • Article Type: Review Article
This is a required field
Please enter a valid email address
Approval was a Success
Invalid data
An Error Occurred
Approval was partially successful, following selected items could not be processed due to error