A Role for Rev-erb alpha Ligands in the Regulation of Adipogenesis

作者：Kojetin Douglas J; Burris Thomas P^*

来源：Current Pharmaceutical Design, 2011, 17(4): 320-324.

DOI：10.2174/138161211795164211

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

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.

• 出版日期2011-2