Yeast Two-hybrid Based Screen For PPARg Agonist And Antagonist

Type-Ⅱdiabetes mellitus is a chronic metabolism disease, characterized by insulin resistance and insulin secretion weakening, which is now afflicting more and more people in the world. Peroxisome proliferator-activated receptors (PPARs) are new members of the nulear receptor family playing a central role in the regulation of storage and catabolism of dietary fats and glucose. Among three subtypes of PPAR, PPARγis most focused and has been developed as an important therapeutic drug target against several diseases such as inflammation, dyslipidemia, hypertension and cancer,especially against Type-Ⅱdiabetes mellitus. In this report, we exploited an efficient approach for discovery of PPARγagonist and antagonist via yeast two-hybrid system based on the fact that PPARγinteracts with the coactivator CBP ligand-dependently. With this built screening platform, four types of PPARγagonists...