Glucocorticoid receptor inhibits transforming growth factor-beta signaling by directly targeting the transcriptional activation function of Smad3

Proc Natl Acad Sci U S A. 1999 Oct 12;96(21):11776-81. doi: 10.1073/pnas.96.21.11776.

Abstract

The transforming growth factor-beta (TGF-beta) family of cytokines and glucocorticoids regulate diverse biological processes through modulating the expression of target genes. Here we report that glucocorticoid receptor (GR) represses TGF-beta transcriptional activation of the type-1 plasminogen activator inhibitor (PAI-1) gene in a ligand-dependent manner. Similarly, GR represses TGF-beta activation of the TGF-beta responsive sequence containing Smad3/4-binding sites. Using mammalian two-hybrid assays, we demonstrate that GR inhibits transcriptional activation by both Smad3 and Smad4 C-terminal activation domains. Finally, we show that GR interacts with Smad3 both in vitro and in vivo. These results suggest a molecular basis for the cross-regulation between glucocorticoid and TGF-beta signaling pathways.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • COS Cells
  • DNA-Binding Proteins / genetics*
  • DNA-Binding Proteins / metabolism
  • Dexamethasone / pharmacology
  • Genes, Reporter
  • Glucocorticoids / pharmacology
  • Humans
  • Luciferases / metabolism
  • Plasmids / metabolism
  • Plasminogen Activator Inhibitor 1 / genetics*
  • Plasminogen Activator Inhibitor 1 / metabolism
  • Precipitin Tests
  • Protein Binding
  • Receptors, Glucocorticoid / genetics*
  • Receptors, Glucocorticoid / metabolism
  • Recombinant Fusion Proteins / metabolism
  • Signal Transduction*
  • Smad3 Protein
  • Trans-Activators / genetics*
  • Trans-Activators / metabolism
  • Transcriptional Activation*
  • Transfection
  • Transforming Growth Factor beta / antagonists & inhibitors
  • Transforming Growth Factor beta / genetics*
  • Tumor Cells, Cultured

Substances

  • DNA-Binding Proteins
  • Glucocorticoids
  • Plasminogen Activator Inhibitor 1
  • Receptors, Glucocorticoid
  • Recombinant Fusion Proteins
  • SMAD3 protein, human
  • Smad3 Protein
  • Trans-Activators
  • Transforming Growth Factor beta
  • Dexamethasone
  • Luciferases