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Updated: Jun 8, 2026

Simultaneous Measurement of HDAC1 and HDAC6 Activity in HeLa Cells Using UHPLC-MS
Published on: August 10, 2017
[Development of HDAC inhibitors]
1Dept. of Molecular-Targeting Cancer Prevention, Kyoto Prefectural University of Medicine, Kamigyo-ku, Kyoto, Japan.
Abstract:
In the mechanisms of carcinogenesis, it is becoming apparent that not only genetic abnormalities including DNA mutations, but also epigenetic abnormalities are heavily involved. Simultaneously, certain kinds of compounds indicated anti-tumor activity through their epigenetic effects. Typical drugs, which have the epigenetic effects, are histone deacetylase(HDAC) inhibitors. So far, two types of HDAC inhibitors, vorinostat and romidepsin, are approved by the Food Drug Administration for cutaneous T-cell lymphoma in the U. S. A. Not only these two compounds but also many HDAC inhibitors are under clinical trials in monotherapy and combination therapy. For a better outcome, it is very important to establish the appropriate biomarkers and appropriate combination based on mode-of-action for HDAC inhibitors, similar to other molecular-target antitumor drugs.
Insights
Epigenetic abnormalities play a key role in cancer development. Histone deacetylase (HDAC) inhibitors are a promising class of anti-tumor drugs with epigenetic effects, showing potential in clinical trials.
Area of Science:
- Oncology
- Epigenetics
- Molecular Biology
Context:
- Carcinogenesis involves both genetic and epigenetic abnormalities.
- Epigenetic modifications are increasingly recognized as crucial in cancer development.
- Histone deacetylase (HDAC) inhibitors represent a class of compounds with demonstrated anti-tumor activity via epigenetic mechanisms.
Purpose:
- To review the role of epigenetic abnormalities in carcinogenesis.
- To highlight the therapeutic potential of histone deacetylase (HDAC) inhibitors.
- To emphasize the need for biomarkers and combination strategies for HDAC inhibitors.
Summary:
- Epigenetic abnormalities, alongside genetic mutations, are integral to cancer mechanisms.
- Histone deacetylase (HDAC) inhibitors, such as vorinostat and romidepsin, exert anti-tumor effects through epigenetic modulation.
- Several HDAC inhibitors are in clinical trials for monotherapy and combination treatments, building on FDA-approved drugs for cutaneous T-cell lymphoma.
Impact:
- Establishes the significance of epigenetic factors in cancer.
- Identifies HDAC inhibitors as a key therapeutic strategy.
- Underscores the importance of personalized medicine approaches, including biomarker identification and optimized combination therapies, for maximizing the efficacy of HDAC inhibitors in cancer treatment.
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