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This version published online on November 1, 2007
Molecular Endocrinology, doi:10.1210/me.2007-0190
A more recent version of this article appeared on February 1, 2008
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Submitted on April 16, 2007
Accepted on October 15, 2007

Identification and characterization of a selective PPAR{beta}/{delta} (NR1C2) antagonist

Barry G. Shearer, David J. Steger, James M. Way, Thomas B. Stanley, David C. Lobe, Didier A. Grillot, Marie A. Iannone, Mitchell A. Lazar, Timothy M. Willson, and Andrew N. Billin*

GlaxoSmithKline, Research and Development, Research Triangle Park, NC 27709 USA; GlaxoSmithKline, Research and Development, Les Ulis, France; Division of Endocrinology, Diabetes, and Metabolism, Department of Medicine, The Institute for Diabetes, Obesity, and Metabolism, University of Pennsylvania School of Medicine, Philadelphia, PA 19104, USA

* To whom correspondence should be addressed. E-mail: andrew.n.billin{at}GSK.com.

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 PPAR{alpha} or PPAR{gamma}. The comparison of these agonist and antagonist ligands in cellular and animal systems has often lead to surprising results and new insights into the biology of the PPARs. The PPAR{beta}/{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 PPAR{beta}/{delta} small molecule antagonist ligand. This antagonist ligand will be a useful tool for elucidating the biological roles of PPAR{beta}/{delta}.
Key words: PPAR • antagonist • ligand

NURSA Molecule Pages Link:

Nuclear Receptors:   PPARδ
Ligands:   GW0742X



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[Abstract] [Full Text] [PDF]


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