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Updated: Jun 29, 2026

Assays for Validating Histone Acetyltransferase Inhibitors

Assays for Validating Histone Acetyltransferase Inhibitors

Published on: August 6, 2020

Histone deacetylase inhibitors: anticancer compounds.

Karen T Smith¹, Jerry L Workman

¹Stowers Institute for Medical Research, Kansas City, MO 64110, USA.

The International Journal of Biochemistry & Cell Biology

|October 11, 2008

Summary

Histone deacetylase inhibitors are promising cancer treatments. These drugs target aberrant epigenetic changes in tumors, inducing cancer cell death or differentiation with minimal toxicity to healthy cells.

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Assays for Validating Histone Acetyltransferase Inhibitors

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

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Purification of H3 and H4 Histone Proteins and the Quantification of Acetylated Histone Marks in Cells and Brain Tissue

Purification of H3 and H4 Histone Proteins and the Quantification of Acetylated Histone Marks in Cells and Brain Tissue

Published on: November 30, 2018

Area of Science:

Biochemistry
Epigenetics
Molecular Biology

Background:

Protein acetylation, regulated by histone acetyltransferases and histone deacetylases, impacts gene expression and protein function.
Aberrant epigenetic modifications, particularly histone deacetylase imbalances, are linked to cancer development.
Histone deacetylase inhibitors are emerging as a therapeutic strategy for various cancers.

Purpose of the Study:

To explore the role of histone deacetylases in cancer.
To review the therapeutic potential of histone deacetylase inhibitors in oncology.

Main Methods:

Review of literature on protein acetylation and histone deacetylases.
Analysis of the mechanisms of action for histone deacetylase inhibitors.
Examination of clinical trial data for histone deacetylase inhibitors in cancer treatment.

Main Results:

Histone acetylation levels correlate with gene activity, with hypoacetylation linked to gene repression.
Non-histone protein acetylation affects protein activity and stability.
Histone deacetylase inhibitors show potential in inducing cancer cell cycle arrest, apoptosis, and differentiation.

Conclusions:

Histone deacetylase inhibitors represent a targeted approach to cancer therapy.
These inhibitors offer a favorable therapeutic window due to limited toxicity in normal cells.
Further clinical investigation of histone deacetylase inhibitors is warranted for diverse cancer types.