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Updated: Jun 12, 2026

Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
[Histone deacetylase inhibitors: highlight on epigenetic regulation]
N Pécuchet1, T Cluzeau, C Thibault
1Groupe hospitalier Pitié-Salpêtrière, Service d'oncologie médicale, 75013 Paris, France.
Abstract:
HDAC, by modifiing relations between DNA and histones, are major proteins of the epigenetic regulation. They play part in the signal transduction and in many cellular processes: cell cycle control, apoptosis, protein degradation, angiogenesis, invasion and cell motility. In several models of cancer HDAC inhibitors (HDACIs) are able to up regulate tumor suppressing gene (p53, p21, pRB...) and to down regulate oncogenes (SRC, HIF-Ialpha,HER2...). Many inhibitors are currently in clinical development and promising results have been reported in cutaneous T cell lymphoma, Hodgkin's disease and non-hodgkin lymphoma. Combination with chemotherapy and molecular targeted agents seem to be effective in myeloma, lung cancer and myeloïd neoplasms. In this review, we focus on recent biologic and clinical data that highlitght the anti-neoplastic role of HDACIs.
Insights
Histone deacetylase (HDAC) inhibitors are epigenetic regulators showing anti-cancer potential by modulating gene expression. Clinical trials reveal promising results, especially in lymphomas and in combination therapies.
Area of Science:
- Epigenetics and Gene Regulation
- Molecular Biology
- Cancer Biology
Context:
- Histone deacetylases (HDACs) are key epigenetic regulators influencing DNA-histone interactions.
- HDACs are involved in critical cellular processes including cell cycle control, apoptosis, and angiogenesis.
- Dysregulation of HDACs is implicated in various cancers.
Purpose:
- To review recent biological and clinical data on the anti-neoplastic role of HDAC inhibitors (HDACIs).
- To highlight the therapeutic potential of HDACIs in cancer treatment.
Summary:
- HDAC inhibitors (HDACIs) modulate gene expression, upregulating tumor suppressors and downregulating oncogenes.
- HDACIs demonstrate efficacy in preclinical cancer models.
- Clinical development shows promising results for HDACIs in lymphomas and in combination therapies for myeloma, lung cancer, and myeloid neoplasms.
Impact:
- HDACIs represent a promising class of anti-cancer agents.
- Combination strategies involving HDACIs may enhance therapeutic outcomes.
- Further clinical investigation of HDACIs is warranted for various malignancies.
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