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Identification and Characterization of a Selective Peroxisome Proliferator-Activated Receptor β/ (NR1C2) Antagonist

GlaxoSmithKline (B.G.S., J.M.W., T.B.S., D.C.L., M.A.I., T.M.W., A.N.B.), Research and Development, Research Triangle Park, North Carolina 27709; GlaxoSmithKline (D.A.G.), Research and Development, 91951 Les Ulis, France; and Division of Endocrinology, Diabetes, and Metabolism (D.J.S., M.A.L.), Department of Medicine, The Institute for Diabetes, Obesity, and Metabolism, University of Pennsylvania School of Medicine, Philadelphia, Pennsylvania 19104

Address all correspondence and requests for reprints to: Andrew N. Billin, GlaxoSmithKline, Research and Development, Research Triangle Park, North Carolina 27709. E-mail: andrew.n.billin{at}GSK.com.

ABSTRACT

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 or PPAR. 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 PPARβ/ 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 PPARβ/ small molecule antagonist ligand. This antagonist ligand will be a useful tool for elucidating the biological roles of PPARβ/.

NURSA Molecule Pages Link:

Nuclear Receptors:   PPARδ

Ligands:   GW0742X