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A role for rev-erb alpha ligands in the regulation of adipogenesis

Academic Article
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Overview

authors

  • Kojetin, Douglas
  • Burris, Thomas

publication date

  • February 2011

journal

  • Current Pharmaceutical Design  Journal

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.

subject areas

  • Adipogenesis
  • Circadian Rhythm
  • Drug Design
  • Gene Expression Regulation
  • Heme
  • Humans
  • Ligands
  • Molecular Targeted Therapy
  • Nuclear Receptor Subfamily 1, Group D, Member 1
  • Transcription, Genetic
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Research

keywords

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

International Standard Serial Number (ISSN)

  • 1381-6128

Digital Object Identifier (DOI)

  • 10.2174/138161211795164211

PubMed ID

  • 21375499
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Additional Document Info

start page

  • 320

end page

  • 324

volume

  • 17

issue

  • 4

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