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Updated: Aug 11, 2026

Assays for Validating Histone Acetyltransferase Inhibitors
09:11

Assays for Validating Histone Acetyltransferase Inhibitors

Published on: August 6, 2020

Histone deacetylase inhibitors: multifunctional anticancer agents

Tao Liu1, Selena Kuljaca, Andrew Tee

  • 1Children's Cancer Institute, Australia for Medical Research, Sydney Children's Hospital, High Street, Randwick, NSW 2031, Australia.

Cancer Treatment Reviews
|March 7, 2006
PubMed

Insights

Histone deacetylase inhibitors (HDACIs) show anti-cancer effects by up-regulating tumor suppressor genes and inhibiting cancer cell migration and metastasis. Further investigation into HDACIs for high-risk cancer patients is warranted.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Cancer Research

Background:

  • Histone deacetylase (HDAC) regulates gene expression through chromatin acetylation.
  • Histone hypo-acetylation is linked to repressed tumor suppressor gene expression.
  • HDAC inhibitors (HDACIs) are emerging as potent anti-cancer agents.

Purpose of the Study:

  • To review the role of HDACIs in cancer, focusing on their impact beyond gene expression.
  • To summarize evidence on HDACIs' effects on cancer cell migration, invasion, metastasis, and angiogenesis.
  • To explore the potential of HDACIs in preventing and treating various cancers.

Main Methods:

  • Literature review of preclinical and clinical studies on HDACIs.
  • Analysis of data on HDACIs' effects on histone and non-histone protein acetylation.
  • Examination of evidence linking HDACIs to suppression of cancer hallmarks.

Main Results:

  • HDACIs effectively up-regulate tumor suppressor genes, reduce tumor growth, and induce apoptosis.
  • HDACI efficacy is partly attributed to suppressing cancer cell migration, invasion, and metastasis.
  • HDACIs also impact angiogenesis and blood supply in tumors.
  • HDACIs demonstrate anti-cancer effects through both histone and non-histone protein acetylation.

Conclusions:

  • HDACIs possess significant anti-cancer properties, extending to the suppression of tumor initiation and progression.
  • The anti-cancer efficacy of HDACIs in vivo is significantly influenced by their ability to inhibit cancer cell migration and metastasis.
  • HDACIs represent a promising therapeutic strategy for various hematological and solid malignancies, including precancerous conditions.

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