Glucocorticoid signaling is perturbed by the atypical orphan receptor and corepressor SHP

J Biol Chem. 2002 Dec 20;277(51):49761-6. doi: 10.1074/jbc.M205641200. Epub 2002 Sep 24.

Abstract

SHP (NROB2) is an atypical orphan nuclear receptor that lacks a DNA-binding domain but contains a putative ligand-binding domain. Previous studies have revealed that SHP interacts with a variety of nuclear receptors and inhibits their transcriptional activity, thereby acting as a corepressor. In this report we identify the glucocorticoid receptor (GR) as a novel downstream target receptor for SHP inhibition. SHP potently inhibits dexamethasone-induced transcriptional GR activity in mammalian cells, and the inhibition involves a functional second NR-box within SHP. Interestingly, this motif shows a high homology with the NR-box in the glucocorticoid and cAMP-inducible GR coactivator PGC-1, indicating similar binding specificity and shared target receptors. We show that SHP antagonizes PGC-1 coactivation and, in addition, we identify the PGC- 1-regulated phospho(enol)pyruvate carboxykinase (PEPCK) promoter as a novel target promoter for SHP inhibition. This implies a physiologically relevant role for SHP in modulating hepatic glucocorticoid action. Furthermore, when coexpressing green fluorescent protein-tagged GR together with SHP, an intranuclear redistribution of GR was observed. As inhibition-deficient SHP mutants were unable to induce this redistribution, intranuclear tethering of target receptors may represent yet another, previously uncovered, aspect of SHP inhibition.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Animals
  • COS Cells
  • Cell Line
  • Cyclic AMP / metabolism
  • Glucocorticoids / metabolism*
  • Glucose / metabolism
  • Green Fluorescent Proteins
  • Humans
  • Liver / metabolism
  • Luminescent Proteins / metabolism
  • Models, Genetic
  • Molecular Sequence Data
  • Mutation
  • Pancreas / metabolism
  • Phosphoenolpyruvate Carboxykinase (GTP) / genetics
  • Plasmids / metabolism
  • Precipitin Tests
  • Promoter Regions, Genetic
  • Protein Binding
  • Protein Structure, Tertiary
  • Receptors, Cytoplasmic and Nuclear / chemistry*
  • Receptors, Cytoplasmic and Nuclear / metabolism*
  • Receptors, Cytoplasmic and Nuclear / physiology
  • Sequence Homology, Amino Acid
  • Signal Transduction*
  • Transcription, Genetic
  • Transfection

Substances

  • Glucocorticoids
  • Luminescent Proteins
  • Receptors, Cytoplasmic and Nuclear
  • nuclear receptor subfamily 0, group B, member 2
  • Green Fluorescent Proteins
  • Cyclic AMP
  • Phosphoenolpyruvate Carboxykinase (GTP)
  • Glucose