Phosphorylation of histone H3T6 by PKCbeta(I) controls demethylation at histone H3K4

Nature. 2010 Apr 1;464(7289):792-6. doi: 10.1038/nature08839. Epub 2010 Mar 14.

Abstract

Demethylation at distinct lysine residues in histone H3 by lysine-specific demethylase 1 (LSD1) causes either gene repression or activation. As a component of co-repressor complexes, LSD1 contributes to target gene repression by removing mono- and dimethyl marks from lysine 4 of histone H3 (H3K4). In contrast, during androgen receptor (AR)-activated gene expression, LSD1 removes mono- and dimethyl marks from lysine 9 of histone H3 (H3K9). Yet, the mechanisms that control this dual specificity of demethylation are unknown. Here we show that phosphorylation of histone H3 at threonine 6 (H3T6) by protein kinase C beta I (PKCbeta(I), also known as PRKCbeta) is the key event that prevents LSD1 from demethylating H3K4 during AR-dependent gene activation. In vitro, histone H3 peptides methylated at lysine 4 and phosphorylated at threonine 6 are no longer LSD1 substrates. In vivo, PKCbeta(I) co-localizes with AR and LSD1 on target gene promoters and phosphorylates H3T6 after androgen-induced gene expression. RNA interference (RNAi)-mediated knockdown of PKCbeta(I) abrogates H3T6 phosphorylation, enhances demethylation at H3K4, and inhibits AR-dependent transcription. Activation of PKCbeta(I) requires androgen-dependent recruitment of the gatekeeper kinase protein kinase C (PKC)-related kinase 1 (PRK1). Notably, increased levels of PKCbeta(I) and phosphorylated H3T6 (H3T6ph) positively correlate with high Gleason scores of prostate carcinomas, and inhibition of PKCbeta(I) blocks AR-induced tumour cell proliferation in vitro and cancer progression of tumour xenografts in vivo. Together, our data establish that androgen-dependent kinase signalling leads to the writing of the new chromatin mark H3T6ph, which in consequence prevents removal of active methyl marks from H3K4 during AR-stimulated gene expression.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Androgens / metabolism
  • Androgens / pharmacology
  • Animals
  • Cell Division / drug effects
  • Cell Line, Tumor
  • Chromatin / metabolism
  • Gene Expression Regulation / drug effects
  • Gene Knockdown Techniques
  • Histone Demethylases / antagonists & inhibitors
  • Histone Demethylases / metabolism*
  • Histones / chemistry*
  • Histones / metabolism*
  • Humans
  • Lysine / chemistry
  • Lysine / metabolism
  • Male
  • Methylation / drug effects
  • Mice
  • Mice, Nude
  • Mice, SCID
  • Phosphorylation / drug effects
  • Phosphothreonine / metabolism
  • Promoter Regions, Genetic / genetics
  • Prostatic Neoplasms / enzymology
  • Prostatic Neoplasms / metabolism
  • Prostatic Neoplasms / pathology
  • Protein Kinase C / antagonists & inhibitors
  • Protein Kinase C / deficiency
  • Protein Kinase C / genetics
  • Protein Kinase C / metabolism*
  • Protein Kinase C beta
  • Signal Transduction / drug effects
  • Xenograft Model Antitumor Assays

Substances

  • Androgens
  • Chromatin
  • Histones
  • Phosphothreonine
  • Histone Demethylases
  • KDM1A protein, human
  • Protein Kinase C
  • Protein Kinase C beta
  • Lysine