cis-Parinaric acid is a ligand for the human peroxisome proliferator activated receptor γ: development of a novel spectrophotometry assay for the discovery of PPARγ ligands

Peroxisome proliferator activated reporter γ(PPARγ) is the subject of intense investigation as a target for drugs against diabetes, atherosclerosis and cancer. For this reason there is considerable interest in the spectrum of compounds that bind this receptor. In this paper we have identified cis-parinaric acid (CPA) as a novel hPPARγ ligand. The binding of this fatty acid to the receptor increases its fluorescence and causes a shift in the UV spectrum. This spectral shift is reversible by competition with other known ligands for PPARγ. This report represents the first direct demonstration of a fatty acid binding to PPARγ.