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Updated: Oct 14, 2026

Simultaneous Measurement of HDAC1 and HDAC6 Activity in HeLa Cells Using UHPLC-MS
09:20

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Published on: August 10, 2017

Inhibition of histone deacetylases: a new strategy to target epigenetic modifications for anticancer treatment

U H Weidle1, A Grossmann

  • 1Roche Diagnostics GmbH, Penzberg, Germany. Ulrich.Weidle@roche.com

Anticancer Research
|August 6, 2000
PubMed

Insights

Histone deacetylase (HDAC) inhibitors, often from natural sources, show promise in cancer treatment by regulating gene expression, cell-cycle arrest, and apoptosis. Further research into HDAC mechanisms is crucial for optimized cancer therapies.

Area of Science:

  • Epigenetics
  • Cancer Biology
  • Pharmacology

Background:

  • Epigenetic modifications, specifically nucleosome acetylation, are implicated in cancer etiology and progression.
  • Histone deacetylases (HDACs) are key enzymes mediating these epigenetic changes.
  • HDACs comprise at least two subfamilies with at least 7 members in mammals.

Purpose of the Study:

  • To discuss the role of epigenetic modifications in cancer.
  • To review natural source-derived histone deacetylase inhibitors (HDACis).
  • To explore the potential of HDACis as antineoplastic agents.

Main Methods:

  • Review of literature on HDAC inhibitors.
  • Analysis of physiological consequences in cancer-related systems (in vitro and in vivo).
  • Assessment of preclinical and clinical development stages of HDAC inhibitors.

Main Results:

  • HDAC inhibition can lead to significant transcriptional changes (affecting ~2% of human genes).
  • HDAC inhibition induces cell-cycle arrest, apoptosis, and differentiation in cancer cells.
  • Several natural source-derived HDAC inhibitors are in preclinical and clinical development.

Conclusions:

  • HDAC inhibitors demonstrate potential as anticancer agents.
  • Elucidating molecular mechanisms of HDAC inhibition is vital for therapeutic optimization.
  • Understanding HDAC isoenzyme function and deregulation in cancer is critical for developing targeted therapies.

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