Open AccessIdentification and Characterization of a Selective Peroxisome Proliferator-Activated Receptor β/δ (NR1C2) Antagonist
Author(s) -
Barry G. Shearer,
David J. Steger,
James M. Way,
Thomas B. Stanley,
David C. Lobe,
Didier Grillot,
Marie A. Ian,
Mitchell A. Lazar,
Timothy M. Willson,
Andrew N. Billin
Publication year - 2008
Publication title -
molecular endocrinology
Language(s) - English
Resource type - Journals
eISSN - 1944-9917
pISSN - 0888-8809
DOI - 10.1210/me.2007-0190
Subject(s) - biology , antagonist , agonist , receptor , peroxisome proliferator activated receptor , regulator , peroxisome , microbiology and biotechnology , peroxisome proliferator activated receptor delta , pharmacology , nuclear receptor , biochemistry , transcription factor , gene
The identification of small molecule ligands for the peroxisome proliferator-activated receptors (PPARs) has been instrumental in elucidating their biological roles. In particular, agonists have been the focus of much of the research in the field with relatively few antagonists being described and all of those being selective for PPARalpha or PPARgamma. The comparison of these agonist and antagonist ligands in cellular and animal systems has often led to surprising results and new insights into the biology of the PPARs. The PPARbeta/delta receptor is emerging as an important regulator of energy metabolism, inflammation, and cell growth and differentiation; however, only agonist ligands have been described for this receptor thus far. Here we describe the first report of a PPARbeta/delta small molecule antagonist ligand. This antagonist ligand will be a useful tool for elucidating the biological roles of PPARbeta/delta.