Acetylation of proteins as novel target for antitumor therapy: review article

E Di Gennaro1, F Bruzzese, M Caraglia

  • 1Dipartimento di Oncologia Sperimentale, Istituto Nazionale Tumori Fondazione G. Pascale, Napoli, Italy.

Amino Acids
|August 4, 2004
PubMed

Insights

Histone deacetylase (HDAC) inhibitors show promise as anticancer agents by inducing cancer cell apoptosis. However, the precise mechanisms behind their tumor selectivity are still under investigation, posing a challenge for cancer research.

Area of Science:

  • Molecular Biology
  • Biochemistry
  • Cancer Research

Background:

  • Histone acetylation regulates gene expression, impacting cell proliferation, differentiation, and apoptosis.
  • Aberrant activity of histone acetyltransferases (HATs) and histone deacetylases (HDACs) is implicated in various cancers.
  • HDACs and HATs also modify non-histone proteins, affecting diverse cellular processes.

Purpose of the Study:

  • To explore the anticancer potential of HDAC inhibitors.
  • To investigate the mechanisms underlying HDAC inhibitor-induced cancer cell apoptosis and growth arrest.
  • To address the challenge of understanding the molecular basis for tumor selectivity of HDAC inhibitors.

Main Methods:

  • Review of existing literature on HDAC inhibitors and their mechanisms of action.
  • Analysis of clinical studies involving HDAC inhibitors.
  • Exploration of the role of histone acetylation and non-histone protein targets.

Main Results:

  • HDAC inhibitors demonstrate efficacy in inducing growth arrest and apoptosis in diverse human cancer cells.
  • The observed anti-cancer effects cannot be solely explained by changes in histone acetylation.
  • Ongoing clinical trials are evaluating the therapeutic potential of these agents.

Conclusions:

  • HDAC inhibitors represent a promising class of novel anticancer agents.
  • Further research is needed to elucidate the molecular mechanisms, particularly tumor selectivity, of HDAC inhibitors.
  • Understanding these mechanisms is crucial for advancing cancer therapy.

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