The coactivator role of histone deacetylase 3 in IL-1-signaling involves deacetylation of p65 NF-κB

Nucleic Acids Res. 2013 Jan 7;41(1):90-109. doi: 10.1093/nar/gks916. Epub 2012 Oct 19.

Abstract

Histone deacetylase (HDAC) 3, as a cofactor in co-repressor complexes containing silencing mediator for retinoid or thyroid-hormone receptors (SMRT) and nuclear receptor co-repressor (N-CoR), has been shown to repress gene transcription in a variety of contexts. Here, we reveal a novel role for HDAC3 as a positive regulator of IL-1-induced gene expression. Various experimental approaches involving RNAi-mediated knockdown, conditional gene deletion or small molecule inhibitors indicate a positive role of HDAC3 for transcription of the majority of IL-1-induced human or murine genes. This effect was independent from the gene regulatory effects mediated by the broad-spectrum HDAC inhibitor trichostatin A (TSA) and thus suggests IL-1-specific functions for HDAC3. The stimulatory function of HDAC3 for inflammatory gene expression involves a mechanism that uses binding to NF-κB p65 and its deacetylation at various lysines. NF-κB p65-deficient cells stably reconstituted to express acetylation mimicking forms of p65 (p65 K/Q) had largely lost their potential to stimulate IL-1-triggered gene expression, implying that the co-activating property of HDAC3 involves the removal of inhibitory NF-κB p65 acetylations at K122, 123, 314 and 315. These data describe a novel function for HDAC3 as a co-activator in inflammatory signaling pathways and help to explain the anti-inflammatory effects frequently observed for HDAC inhibitors in (pre)clinical use.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetylation
  • Animals
  • Cell Line
  • Chemokine CXCL2 / genetics
  • Chemokine CXCL2 / metabolism
  • Down-Regulation
  • Histone Deacetylase Inhibitors / pharmacology
  • Histone Deacetylases / physiology*
  • Humans
  • Hydroxamic Acids / pharmacology
  • Interleukin-1 / pharmacology*
  • Interleukin-8 / genetics
  • Interleukin-8 / metabolism
  • Mice
  • NF-kappa B / metabolism
  • Phosphorylation
  • RNA Polymerase II / metabolism
  • Signal Transduction
  • Transcription Factor RelA / metabolism*
  • Transcription, Genetic / drug effects

Substances

  • Chemokine CXCL2
  • Cxcl2 protein, mouse
  • Histone Deacetylase Inhibitors
  • Hydroxamic Acids
  • Interleukin-1
  • Interleukin-8
  • NF-kappa B
  • Transcription Factor RelA
  • trichostatin A
  • RNA Polymerase II
  • Histone Deacetylases
  • histone deacetylase 3