Divalproex sodium modulates nuclear localization of ataxin-3 and prevents cellular toxicity caused by expanded ataxin-3

CNS Neurosci Ther. 2018 May;24(5):404-411. doi: 10.1111/cns.12795. Epub 2018 Jan 9.

Abstract

Background & aims: Spinocerebellar ataxia type 3 (SCA3), also known as Machado-Joseph disease (MJD), is an autosomal dominantly inherited neurodegenerative disorder and the most common form of SCA worldwide. It is caused by the expansion of a polyglutamine (polyQ) tract in the ataxin-3 protein. Nuclear localization of the affected protein is a key event in the pathology of SCA3 via affecting nuclear organization, transcriptional dysfunction, and seeding aggregations, finally causing neurodegeneration and cell death. So far, there is no effective therapy to prevent or slow the progression of SCA3.

Methods: In this study, we explored the effect of divalproex sodium as an HDACi in SCA3 cell models and explored how divalproex sodium interferes with pathogenetic processes causing SCA3.

Results: We found that divalproex sodium rescues the hypoacetylation levels of histone H3 and attenuates cellular cytotoxicity induced by expanded ataxin-3 partly via preventing nuclear transport of ataxin-3 (particularly heat shock-dependent).

Conclusion: Our study provides novel insights into the mechanisms of action of divalproex sodium as a possible treatment for SCA3, beyond the known regulation of transcription.

Keywords: HDAC inhibitors; SCA3 treatment; divalproex sodium; nuclear localization; transcriptional dysfunction.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetylation / drug effects
  • Active Transport, Cell Nucleus / drug effects*
  • Animals
  • Ataxin-3 / metabolism*
  • CHO Cells
  • Cell Survival / drug effects
  • Cell Survival / physiology
  • Cricetulus
  • HEK293 Cells
  • Heat-Shock Response / drug effects
  • Heat-Shock Response / physiology
  • Histones / metabolism
  • Humans
  • Neuroprotective Agents / pharmacology*
  • Protein Aggregates / drug effects
  • Repressor Proteins / metabolism*
  • Valproic Acid / pharmacology*

Substances

  • Histones
  • Neuroprotective Agents
  • Protein Aggregates
  • Repressor Proteins
  • Valproic Acid
  • ATXN3 protein, human
  • Ataxin-3