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Updated: May 26, 2026

Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
Histone acetyltransferases and deacetylases: molecular and clinical implications to gastrointestinal carcinogenesis
Wei-Jian Sun1, Xiang Zhou, Ji-Hang Zheng
1The 2nd Affiliated Hospital, Wenzhou Medical College, China.
Abstract:
Histone acetyltransferases and deacetylases are two groups of enzymes whose opposing activities govern the dynamic levels of reversible acetylation on specific lysine residues of histones and many other proteins. Gastrointestinal (GI) carcinogenesis is a major cause of morbidity and mortality worldwide. In addition to genetic and environmental factors, the role of epigenetic abnormalities such as aberrant histone acetylation has been recognized to be pivotal in regulating benign tumorigenesis and eventual malignant transformation. Here we provide an overview of histone acetylation, list the major groups of histone acetyltransferases and deacetylases, and cover in relatively more details the recent studies that suggest the links of these enzymes to GI carcinogenesis. As potential novel therapeutics for GI and other cancers, histone deacetylase inhibitors are also discussed.
Insights
Histone acetylation, regulated by enzymes like histone acetyltransferases and deacetylases, plays a key role in gastrointestinal (GI) carcinogenesis. Histone deacetylase inhibitors show promise as novel cancer therapeutics.
Area of Science:
- Biochemistry
- Molecular Biology
- Oncology
Background:
- Gastrointestinal (GI) carcinogenesis is a significant global health concern.
- Epigenetic alterations, particularly aberrant histone acetylation, are increasingly recognized in cancer development.
- Histone acetyltransferases (HATs) and histone deacetylases (HDACs) dynamically regulate protein acetylation.
Purpose of the Study:
- To provide an overview of histone acetylation.
- To identify major groups of HATs and HDACs.
- To explore the link between these enzymes and GI carcinogenesis.
Main Methods:
- Literature review of histone acetylation.
- Overview of HAT and HDAC enzyme families.
- Analysis of recent studies on enzyme roles in GI cancer.
Main Results:
- Histone acetylation is a critical epigenetic mechanism in GI tumorigenesis.
- Specific HATs and HDACs are implicated in the progression of GI cancers.
- Histone deacetylase inhibitors (HDACis) are emerging as potential therapeutic agents.
Conclusions:
- Aberrant histone acetylation is pivotal in GI carcinogenesis.
- Targeting HATs and HDACs offers a promising therapeutic strategy for GI cancers.
- HDAC inhibitors represent a novel class of drugs for cancer treatment.
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