Pharmacological Inhibition of O-GlcNAcase Does Not Increase Sensitivity of Glucocorticoid Receptor-Mediated Transrepression

PLoS One. 2015 Dec 15;10(12):e0145151. doi: 10.1371/journal.pone.0145151. eCollection 2015.

Abstract

Glucocorticoid signaling regulates target genes by multiple mechanisms, including the repression of transcriptional activities of nuclear factor κ-light-chain-enhancer of activated B cells (NF-κB) though direct protein-protein interactions and subsequent O-GlcNAcylation of RNA polymerase II (pol II). Recent studies have shown that overexpression of O-linked β-N-acetylglucosamine transferase (OGT), which adds an O-linked β-N-acetylglucosamine (O-GlcNAc) group to the C-terminal domain of RNA pol II, increases the transrepression effects of glucocorticoids (GC). As O-GlcNAcase (OGA) is an enzyme that removes O-GlcNAc from O-GlcNAcylated proteins, we hypothesized that the potentiation of GC effects following OGT overexpression could be similarly observed via the direct inhibition of OGA, inhibiting O-GlcNAc removal from pol II. Here we show that despite pharmacological evidence of target engagement by a selective small molecule inhibitor of OGA, there is no evidence for a sensitizing effect on glucocorticoid-mediated effects on TNF-α promoter activity, or gene expression generally, in human cells. Furthermore, inhibition of OGA did not potentiate glucocorticoid-induced apoptosis in several cancer cell lines. Thus, despite evidence for O-GlcNAc modification of RNA pol II in GR-mediated transrepression, our data indicate that pharmacological inhibition of OGA does not potentiate or enhance glucocorticoid-mediated transrepression.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Apoptosis / drug effects
  • Apoptosis / genetics
  • Dexamethasone / pharmacology
  • Enzyme Inhibitors / pharmacology*
  • Gene Expression Profiling
  • Gene Expression Regulation, Neoplastic / drug effects
  • Humans
  • Inflammation / genetics
  • Inhibitory Concentration 50
  • Leukocytes, Mononuclear / drug effects
  • Leukocytes, Mononuclear / metabolism
  • Lipopolysaccharides / pharmacology
  • N-Acetylglucosaminyltransferases / antagonists & inhibitors*
  • N-Acetylglucosaminyltransferases / metabolism
  • Prednisolone / pharmacology
  • Pyrans / pharmacology*
  • Receptors, Glucocorticoid / metabolism*
  • Thiazoles / pharmacology*
  • Tumor Necrosis Factor-alpha / pharmacology
  • U937 Cells

Substances

  • Enzyme Inhibitors
  • Lipopolysaccharides
  • Pyrans
  • Receptors, Glucocorticoid
  • Thiazoles
  • Tumor Necrosis Factor-alpha
  • thiamet G
  • Dexamethasone
  • Prednisolone
  • N-Acetylglucosaminyltransferases
  • UDP-N-acetylglucosamine-peptide beta-N-acetylglucosaminyltransferase

Grants and funding

The work was funded entirely by Merck & Co., Inc. The funder provided support in the form of salaries for authors PS, LH, AH, HM, MM, PS, MS, DZ, IZ, PB, but did not have any additional role in the study design, data collection and analysis, decision to publish, or preparation of the manuscript. The specific roles of these authors are articulated in the ‘author contributions’ section.