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

FEBS Letters

Palmer, Colin N.A¹  Wolf, C.Roland¹ 

[1] Biomedical Research Centre and ICRF Molecular Pharmacology Unit, Ninewells Hospital and Medical School, University of Dundee, Dundee, DD1 9SY, UK

关键词: Peroxisome proliferator;    Anti-diabetes drug;    Fatty acid;    Fluorescence;    Spectrophotometry;    Nuclear receptor;   

DOI  :  10.1016/S0014-5793(98)00818-7

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

Peroxisome proliferator activated receptor 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.

【 授权许可】

Unknown