Epigenetics and therapeutic targets in gastrointestinal malignancies
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Updated: Nov 8, 2025

Genome-Wide Analysis of DNA Methylation in Gastrointestinal Cancer
Published on: September 18, 2020
Ganji Purnachandra Nagaraju1, Prameswari Kasa2, Begum Dariya3
1Department of Hematology & Medical Oncology, Winship Cancer Institute, Emory University, Atlanta, GA 30332, USA.
Abstract:
Gastrointestinal (GI) malignancies account for substantial mortality and morbidity worldwide. They are generally promoted by dysregulated signal transduction and epigenetic pathways, which are controlled by specific enzymes. Recent studies demonstrated that histone deacetylases (HDACs) together with DNA methyltransferases (DNMTs) have crucial roles in the signal transduction/epigenetic pathways in GI regulation. In this review, we discuss various enzyme targets and their functional mechanisms responsible for the regulatory processes of GI malignancies. We also discuss the epigenetic therapeutic targets that are mainly facilitated by DNMT and HDAC inhibitors, which have functional consequences and clinical outcomes for GI malignancies.
Insights
This review explores enzyme targets in gastrointestinal (GI) malignancies, focusing on histone deacetylases (HDACs) and DNA methyltransferases (DNMTs). It discusses epigenetic therapies using HDAC and DNMT inhibitors for GI cancer treatment.
Area of Science:
- Oncology
- Epigenetics
- Molecular Biology
Background:
- Gastrointestinal (GI) malignancies contribute significantly to global mortality and morbidity.
- Dysregulated signal transduction and epigenetic pathways, controlled by enzymes, promote GI cancers.
- Histone deacetylases (HDACs) and DNA methyltransferases (DNMTs) play critical roles in GI regulation.
Purpose of the Study:
- To review enzyme targets and their mechanisms in GI malignancy regulation.
- To discuss epigenetic therapeutic targets, particularly DNMT and HDAC inhibitors.
- To examine the clinical outcomes of these epigenetic therapies in GI malignancies.
Main Methods:
- Literature review of studies on enzyme targets in GI malignancies.
- Analysis of functional mechanisms of HDACs and DNMTs in GI cancer.
- Evaluation of clinical data on DNMT and HDAC inhibitors for GI malignancies.
Main Results:
- HDACs and DNMTs are key regulators in GI cancer development.
- Epigenetic inhibitors targeting DNMTs and HDACs show therapeutic potential.
- These inhibitors have demonstrated functional consequences and clinical outcomes in GI malignancies.
Conclusions:
- Enzyme targets like HDACs and DNMTs are crucial in GI malignancies.
- Epigenetic therapies offer promising avenues for GI cancer treatment.
- Further research into DNMT and HDAC inhibitors is warranted for improved clinical outcomes.
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