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Updated: Jun 24, 2026

Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
HDACi--targets beyond chromatin
Marc Buchwald1, Oliver H Krämer, Thorsten Heinzel
1Center for Molecular Biomedicine, Institute for Biochemistry and Biophysics, Friedrich-Schiller-Universität Jena, Jena, Germany. Marc.Buchwald@uni-jena.de
Abstract:
Histone deacetylases (HDACs) play an important role in gene regulation. Inhibitors of HDACs (HDACi) are novel anti-cancer drugs, which induce histone (hyper-) acetylation and counteract aberrant gene repression. On the other hand, HDACi treatment can also result in decreased gene expression, and targeting HDACs affects more than chromatin. Recently, HDACi were shown to evoke non-histone protein acetylation, which can alter signaling networks relevant for tumorgenesis. Furthermore, HDACi can promote the degradation of (proto-) oncoproteins. Here, we summarize these findings and discuss how these substances could be beneficial for the treatment and prevention of human ailments, such as cancer and unbalanced immune functions.
Insights
Histone deacetylase inhibitors (HDACi) offer novel anti-cancer strategies by altering gene expression and protein function. These compounds show promise for treating cancer and immune disorders.
Area of Science:
- Biochemistry
- Molecular Biology
- Pharmacology
Background:
- Histone deacetylases (HDACs) are crucial regulators of gene expression through chromatin modification.
- HDAC inhibitors (HDACi) are emerging as therapeutic agents, particularly in oncology.
- HDACi impact gene expression by inducing histone hyperacetylation, counteracting aberrant gene repression.
Purpose of the Study:
- To review the multifaceted roles of HDAC inhibitors beyond chromatin remodeling.
- To explore the effects of HDACi on non-histone protein acetylation and signaling pathways.
- To discuss the potential of HDACi in cancer and immune function regulation.
Main Methods:
- Literature review of studies investigating HDAC inhibitors' mechanisms of action.
- Analysis of research on non-histone protein acetylation induced by HDACi.
- Examination of evidence regarding HDACi's impact on protein degradation pathways.
Main Results:
- HDACi induce both histone and non-histone protein acetylation.
- Non-histone protein acetylation by HDACi can modulate critical signaling networks in tumorgenesis.
- HDACi can promote the degradation of oncoproteins, contributing to anti-cancer effects.
Conclusions:
- HDAC inhibitors possess diverse mechanisms of action, extending beyond chromatin modification.
- HDACi represent a promising therapeutic avenue for cancer treatment.
- Further research into HDACi could yield benefits for managing unbalanced immune functions.
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