[Histone deacetylase inhibitors in the treatment of hematological malignancies]
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Updated: May 30, 2026

Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
Richard Lemal1, Aurélie Ravinet, Cécile Moluçon-Chabrot
1CHU Estaing, service d'hématologie clinique adulte, Clermont-Ferrand Cedex, France.
Abstract:
Histone deacetylases inhibitors (HDACi) represent a new epigenetic targeting therapy class, which is widely investigated in fundamental research and clinical trials. They are able to restore and increase tumor suppressor genes expression and to play an anti-tumoral activity through numerous targets, which are distributed all over the main differentiation, proliferation and survival cellular pathways. Their use in hematology led to vorinostat (SAHA) and romidepsin approval by FDA for the treatment of refractory cutaneous T-cell lymphomas. Preclinical and preliminary clinical results show a promising antineoplasic activity in most hematologic malignancies. This review will focus on the HDACi recent developments and current investigations, highlighted by recent communications.
Insights
Histone deacetylases inhibitors (HDACi) are a promising epigenetic therapy for hematologic malignancies. These drugs restore tumor suppressor genes, showing anti-cancer activity and leading to FDA-approved treatments.
Area of Science:
- Epigenetics and molecular oncology
- Pharmacology of targeted therapies
Context:
- Histone deacetylases inhibitors (HDACi) are an emerging class of epigenetic drugs.
- HDACi are being investigated for their anti-tumoral effects in various cancers.
- Two HDACi, vorinostat and romidepsin, are FDA-approved for refractory cutaneous T-cell lymphomas.
Purpose:
- To review recent developments and current investigations of HDAC inhibitors.
- To highlight the anti-neoplastic activity of HDACi in hematologic malignancies.
- To discuss the molecular mechanisms of HDACi in cellular pathways.
Summary:
- HDAC inhibitors modulate gene expression by targeting histone deacetylases, impacting tumor suppressor genes.
- They exhibit anti-tumoral activity by influencing differentiation, proliferation, and survival pathways.
- Preclinical and clinical data suggest efficacy across a range of hematologic cancers.
Impact:
- HDACi represent a significant advancement in epigenetic cancer therapy.
- Their application in hematology has led to approved treatments and holds promise for other blood cancers.
- Ongoing research continues to explore the therapeutic potential of HDAC inhibitors.
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