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Updated: Jun 13, 2026

Testing Targeted Therapies in Cancer using Structural DNA Alteration Analysis and Patient-Derived Xenografts
Published on: July 25, 2020
Pharmaco-epigenomics: discovering therapeutic approaches and biomarkers for cancer therapy
B Claes1, I Buysschaert, D Lambrechts
1Vesalius Research Center, VIB and K.U. Leuven, Campus Gasthuisberg, Leuven, Belgium.
Abstract:
An important feature of cancer is dysregulation of gene activity and gene expression, which is driven by a combination of acquired genetic and epigenetic alterations. Here, we will highlight how insights into the epigenetic processes underpinning tumor biology have led to the emerging field of cancer pharmaco-epigenomics. First, we will discuss how interference with the epigenetic machinery in cancer is leading to novel promising therapies, with several DNA methyltransferase and histone deacetylase inhibitors being approved for cancer treatment. Second, we will discuss how epigenetic markers in cancer may increasingly be used as complementary diagnostic tools, prognostic markers of disease progression, and predictive markers of treatment response. Although the anti-tumoral activities of epigenetic therapies have thus far been attributed to reactivation of silenced tumor-suppressor and/or apoptotic genes, they may also influence the tumor environment by directly affecting stromal cells. As an example, we will discuss how tumor-endothelial cells are regulated at the epigenetic level and are affected by methyltransferase and histone deacetylase inhibitors.
Insights
Cancer pharmaco-epigenomics leverages epigenetic insights for novel therapies and diagnostics. Epigenetic drugs, like DNA methyltransferase and histone deacetylase inhibitors, show promise in cancer treatment and patient stratification.
Area of Science:
- Oncology
- Epigenetics
- Pharmacology
Background:
- Cancer is characterized by dysregulated gene activity and expression due to genetic and epigenetic alterations.
- Epigenetic processes are increasingly recognized as key drivers of tumor biology and progression.
Purpose of the Study:
- To highlight the emergence of cancer pharmaco-epigenomics.
- To discuss the therapeutic potential of targeting epigenetic machinery in cancer.
- To explore the utility of epigenetic markers in cancer diagnostics and prognostics.
Main Methods:
- Review of current research on epigenetic alterations in cancer.
- Analysis of approved epigenetic therapies, including DNA methyltransferase and histone deacetylase inhibitors.
- Discussion of the role of epigenetic modifications in tumor microenvironment and stromal cells.
Main Results:
- Epigenetic interference offers novel therapeutic strategies, with approved DNA methyltransferase and histone deacetylase inhibitors.
- Epigenetic markers show potential as diagnostic, prognostic, and predictive tools in cancer.
- Epigenetic therapies can impact tumor-stromal interactions, including tumor-endothelial cells.
Conclusions:
- Cancer pharmaco-epigenomics is a rapidly developing field with significant therapeutic and diagnostic implications.
- Targeting epigenetic machinery provides a promising avenue for cancer treatment.
- Epigenetic markers are valuable for personalized cancer care and understanding tumor biology.
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