CIS-PARINARIC ACID IS A LIGAND FOR THE HUMAN PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR-GAMMA - DEVELOPMENT OF A NOVEL SPECTROPHOTOMETRIC ASSAY FOR THE DISCOVERY OF PPAR-GAMMA LIGANDS

Peroxisome proliferator activated receptor gamma (PPAR gamma) is the s ubject of intense investigation as a target for drugs against diabetes , atherosclerosis and cancer. For this reason there is considerable in terest in the spectrum of compounds that bind this receptor. In this p aper,ve have identified cis-parinaric acid (CPA) as a novel hPPAR gamm a ligand. The binding of this fatty acid to the receptor increases its fluorescence and causes a shift in the UV spectrum. This spectral shi ft is reversible by competition with other known ligands for PPAR gamm a. This report represents the first direct demonstration of a fatty ac id binding to PPAR gamma. (C) 1998 Federation of European Biochemical Societies.