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Updated: Jul 1, 2026

Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
[Histone deacetylases: a new class of efficient anti-tumor drugs]
Denis Mottet1, Vincent Castronovo
1Laboratoire de Recherche sur les Métastases, GIGA-Cancer (CRCE), Université de Liège, Tour de Pathologie-1, Building B23, Sart Tilman, 4000 Liège, Belgique. vcastronovo@ulg.ac.be
Abstract:
Circa twenty-five years ago, cancer research was dominated by the concept that the origin of cancer was genetic. Thousands of genetic alterations have indeed been identified involving more than hundred different genes in cancer development. Today, the model has evolved: it has been demonstrated that malignancies can be initiated not only through genetic alterations but also through epigenetic deregulations. By altering the expression of gene involved in cell regulation, epigenetic alterations, such as histone acetylation, play a key role in the initiation and progression of neoplasm. It has been shown that an imbalance between the acelylated and deacetylated status of chromatin is significantly involved in the acquisition of a malignant phenotype. Thus, the modulation of the histone acetylation level by histone deacetylase (HDAC) inhibitors could lead to a genetic re-programmation in cancer cells that would favor apoptosis and prevent proliferation. The potential therapeutic value of several HDAC inhibitors for cancer patients has been evaluated in clinical assays with very promising outcome. Indeed, the first inhibitors available for patients has been recently approved for cancer patients tracing the way for a new class of promising anti-cancer therapy modalities.
Insights
Cancer development involves genetic and epigenetic changes. Histone deacetylase (HDAC) inhibitors reprogram cancer cells, offering a promising new therapeutic approach.
Area of Science:
- Oncology
- Epigenetics
- Molecular Biology
Context:
- Cancer research historically focused on genetic alterations.
- Emerging evidence highlights the role of epigenetic deregulation in malignancy.
- Histone acetylation is a key epigenetic mechanism in cancer initiation and progression.
Purpose:
- To explore the role of epigenetic alterations, specifically histone acetylation, in cancer.
- To investigate histone deacetylase (HDAC) inhibitors as a therapeutic strategy.
- To highlight the potential of HDAC inhibitors in cancer treatment.
Summary:
- Malignancies arise from both genetic mutations and epigenetic changes.
- Epigenetic alterations, like aberrant histone acetylation, drive cancer development.
- Modulating histone acetylation with HDAC inhibitors can reverse malignant phenotypes, promoting apoptosis and inhibiting proliferation.
Impact:
- HDAC inhibitors offer a novel therapeutic avenue for cancer treatment.
- Clinical trials show promising outcomes for HDAC inhibitor-based therapies.
- Recent FDA approvals pave the way for a new class of anti-cancer drugs.
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