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Assays for Validating Histone Acetyltransferase Inhibitors
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Histone deacetylase inhibitors: a new wave of molecular targeted anticancer agents

Alfredo Budillon1, Elena Di Gennaro, Francesca Bruzzese

  • 1Experimental Pharmacology Unit, Department of Experimental Oncology, National Cancer Institute Fondazione G. Pascale, Naples, Italy. budillon@fondazionepascale.it

Recent Patents on Anti-Cancer Drug Discovery
|January 29, 2008
PubMed

Insights

Histone deacetylase (HDAC) inhibitors show promise in cancer therapy by inducing apoptosis. However, their precise anti-cancer mechanisms and tumor selectivity require further investigation.

Area of Science:

  • Oncology
  • Epigenetics
  • Molecular Biology

Background:

  • Epigenetic modifications, including protein acetylation, are crucial in cancer development.
  • Histone acetyltransferases (HATs) and histone deacetylases (HDACs) regulate gene expression and are implicated in various cancers.
  • Altered histone acetylation impacts chromatin structure and the regulation of genes controlling cell proliferation, differentiation, and apoptosis.

Purpose of the Study:

  • To explore the therapeutic potential of targeting epigenetic modifications in anti-cancer strategies.
  • To investigate the role of histone acetylation and non-histone protein acetylation in cancer.
  • To understand the mechanisms and tumor selectivity of HDAC inhibitors.

Main Methods:

  • Review of current research on epigenetic targets in cancer therapy.
  • Analysis of the function of HATs and HDACs in cancer-related pathways.
  • Examination of the effects of HDAC inhibitors on cancer cell lines.

Main Results:

  • HDAC inhibitors have demonstrated the ability to induce growth arrest and apoptosis in diverse human cancer cells.
  • Acetylation affects both histone and non-histone proteins, influencing their function and stability.
  • Several HDAC inhibitors have been patented as potential anti-cancer agents.

Conclusions:

  • HDAC inhibitors represent a promising class of anti-cancer agents.
  • The anti-cancer effects of HDAC inhibitors are not fully explained by histone acetylation alone.
  • Further research is needed to elucidate the molecular mechanisms and tumor selectivity of HDAC inhibitors.

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