Cayman Chemical PPARγ-LBD Ligand Screening Assay Kit

Cayman Chemical’s PPARγ-LBD Ligand Screening Assay Kit provides a convenient fluorescence polarisation-based, single-step assay for screening ligands of the PPARγ-ligand binding domain (PPARγ-LBD). In this assay, a ligand of PPARγ is conjugated to fluorescein and is used as the displacement probe. Free ligands (agonists or antagonists) of the PPARγ-LBD will compete for the high-affinity binding site, displacing the fluorescent probe, which leads to a decrease in fluorescence polarisation. The assay can be used to better understand PPARγ’s mechanism of action and subsequent biological effects, aiding in the identification of next-generation drug candidates in the treatment of metabolic disorders.

The PPAR subfamily of nuclear receptors represents a group of peroxisome proliferators that coordinate the transcriptional activation of genes involved in lipid metabolic pathways. While PPARs display a high degree of homology at the protein level, each subtype exhibits distinct, non-interchangeable roles in energy metabolism that range from energy utilisation to energy storage. The PPARγ subtype is highly expressed in adipose tissue, macrophages and the colon, and has a role in insulin sensitisation, glucose metabolism, lipid metabolism and prevention of oxidative stress. Known ligands for PPARγ include fatty acids and thiazolidinediones such as pioglitazone and rosiglitazone.