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

Author(s): Douglas J. Kojetin, Thomas P. Burris

Journal Name: Current Pharmaceutical Design

Volume 17 , Issue 4 , 2011

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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

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Article Details

Year: 2011
Page: [320 - 324]
Pages: 5
DOI: 10.2174/138161211795164211
Price: $65

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