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A Role for Rev-erbα Ligands in the Regulation of Adipogenesis

[ Vol. 17 , Issue. 4 ]

Author(s):

Douglas J. Kojetin and Thomas P. Burris   Pages 320 - 324 ( 5 )

Abstract:


Rev-erbs are members of the nuclear receptor (NR) transcription factor superfamily and are widely expressed, but are most prevalent in liver, adipose tissue, skeletal muscle and brain. Rev-erbs are key regulators of the circadian rhythm and are expressed in a circadian manner. The discovery that Rev-erbs are ligand-regulated receptors, whose repressive activity is regulated by the endogenous porphyrin ligand, heme, as well as the recent report of the first synthetic Rev-erb ligand, GSK4112/SR6452, suggests that pharmacological modulation through Rev-erb may provide new routes to treat metabolic diseases. Here, we review the work leading to the discovery that Rev-erbs are indeed ligand-regulated and the role that both natural and synthetic Rev-erb ligands have on adipogenesis.

Keywords:

Nuclear receptor, heme, GSK4112, SR6452, adipogenesis, metabolism, diabetes, obesity

Affiliation:

The Scripps Research Institute, 130 Scripps Way 2A1, Jupiter, FL 33458; 561-228-2217.



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