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Assays for Validating Histone Acetyltransferase Inhibitors
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Published on: August 6, 2020

Selective histone deacetylase inhibitors

Huili Pan1, Jiangying Cao, Wenfang Xu

  • 1Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, Ji'nan, Shandong, China.

Anti-Cancer Agents in Medicinal Chemistry
|January 24, 2012
PubMed

Insights

Histone deacetylase inhibitors (HDACi) show anti-cancer potential. This review explores selective HDAC inhibitors, offering a less toxic alternative to pan-HDAC inhibitors by targeting specific subtypes.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Oncology

Background:

  • Histone deacetylases (HDACs) are crucial metalloproteases implicated in cancer development.
  • HDACs comprise 18 subtypes, each with distinct structural characteristics.
  • Existing pan-HDAC inhibitors have advanced to clinical trials for cancer therapy.

Purpose of the Study:

  • To review individual HDAC members and their roles in cancer.
  • To explore the potential of selective HDAC inhibitors as targeted anti-cancer agents.
  • To elucidate the structure-selectivity relationship for developing novel HDAC inhibitors.

Main Methods:

  • Literature review of HDACs and their inhibitors.
  • Analysis of structural diversity among HDAC subtypes.
  • Examination of structure-activity relationships for isoform selectivity.

Main Results:

  • Pan-HDAC inhibitors are widely studied but associated with toxicity.
  • Selective HDAC inhibitors present a promising avenue for reduced toxicity and improved tolerability.
  • Structural modifications are key to achieving isoform-specific inhibition.

Conclusions:

  • Targeting specific HDAC subtypes offers a more precise and potentially safer anti-cancer strategy.
  • Further research into structure-selectivity is essential for developing effective and well-tolerated HDAC inhibitors.
  • Selective HDAC inhibitors represent a significant advancement in targeted cancer therapy.

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