The glucocorticoid receptor is a co-regulator of the orphan nuclear receptor Nurr1

J Neurochem. 2008 Feb;104(3):777-89. doi: 10.1111/j.1471-4159.2007.05055.x. Epub 2007 Nov 6.

Abstract

Nurr1 (NR4A2) is an atypical nuclear receptor (NR) because of its inability to bind a ligand and to activate transcription following canonical NR rules. An affinity chromatography-based screen identified the glucocorticoid receptor (GR) as an interactant of Nurr1. The co-localization of these two NRs in the hippocampus and the substantia nigra, as well as their involvement in similar neurological processes led us to investigate the functional consequences of such a physical interaction. GR interfered with Nurr1 transcriptional activity, and Nurr1 association to GR confers glucocorticoid regulation to this orphan receptor. The N-terminal domain of Nurr1 interacts directly with GR, whereas several domains of GR can associate to Nurr1. The GR-mediated increase in Nurr1 transcriptional activity requires the N-terminal domain of GR, but not a functional DNA binding domain. Finally, SMRT and SRC2, two co-regulators of GR, modulated the transcriptional activity of the Nurr1-GR complex, but not that of Nurr1 alone. Our results therefore establish GR as a transcriptional regulator of Nurr1, and open new opportunities in the pharmacological regulation of Nurr1 by glucocorticoids in the CNS.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adaptor Proteins, Signal Transducing / metabolism
  • Animals
  • Binding Sites
  • DNA-Binding Proteins / metabolism*
  • Hippocampus / metabolism
  • Nuclear Receptor Co-Repressor 2
  • Nuclear Receptor Subfamily 4, Group A, Member 2
  • PC12 Cells
  • Protein Binding
  • Protein Structure, Tertiary
  • Proto-Oncogene Proteins pp60(c-src) / metabolism
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, Glucocorticoid / metabolism*
  • Repressor Proteins / metabolism
  • Substantia Nigra
  • Transcription Factors / metabolism*
  • Transcription, Genetic
  • Transcriptional Activation / physiology*
  • Transfection

Substances

  • Adaptor Proteins, Signal Transducing
  • DNA-Binding Proteins
  • Ncor2 protein, mouse
  • Ncor2 protein, rat
  • Nr4a2 protein, mouse
  • Nr4a2 protein, rat
  • Nuclear Receptor Co-Repressor 2
  • Nuclear Receptor Subfamily 4, Group A, Member 2
  • Receptors, Glucocorticoid
  • Repressor Proteins
  • Sla2 protein, mouse
  • Transcription Factors
  • Proto-Oncogene Proteins pp60(c-src)