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Updated: Apr 27, 2026
Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
Targeting histone deacetylases for cancer therapy: from molecular mechanisms to clinical implications
11. Key Laboratory of Carcinogenesis and Translational Research (Ministry of Education), Beijing 100191, China. ; 2. Department of Biochemistry and Molecular Biology, Peking University Health Science Center, Beijing, 100191, China.
Abstract:
Genetic abnormalities have been conventionally considered as hallmarks of cancer. However, studies over the past decades have demonstrated that epigenetic regulation also participates in the development of cancer. The fundamental patterns of epigenetic components, such as DNA methylation and histone modifications, are frequently altered in tumor cells. Acetylation is one of the best characterized modifications of histones, which is controlled by histone acetyltransferases (HATs) and histone deacetylases (HDACs). HDACs are a group of enzymes which catalyze the removal of the acetyl groups of both histones and non-histone proteins. HDACs are involved in modulating most key cellular processes, including transcriptional regulation, apoptosis, DNA damage repair, cell cycle control, autophagy, metabolism, senescence and chaperone function. Because HDACs have been found to function incorrectly in cancer, various HDAC inhibitors are being investigated to act as cancer chemotherapeutics. The primary purpose of this paper is to summarize recent studies of the links between HDACs and cancer, and further discuss the underlying mechanisms of anti-tumor activities of HDAC inhibitors and clinical implications.
Insights
Histone deacetylases (HDACs) are crucial epigenetic regulators frequently altered in cancer. Inhibitors targeting HDACs show promise as cancer therapeutics by disrupting tumor cell processes.
Area of Science:
- Molecular Biology
- Epigenetics
- Cancer Research
Background:
- Cancer development is linked to genetic abnormalities and epigenetic dysregulation.
- Histone modifications, including acetylation, are key epigenetic mechanisms frequently altered in tumors.
- Histone deacetylases (HDACs) remove acetyl groups, impacting numerous cellular processes.
Purpose of the Study:
- To review recent findings on the role of HDACs in cancer.
- To explore the mechanisms behind the anti-tumor effects of HDAC inhibitors.
- To discuss the clinical relevance of HDAC inhibitors in cancer therapy.
Main Methods:
- Literature review of recent studies on HDACs and cancer.
- Analysis of epigenetic regulation in tumor cells.
- Examination of HDAC inhibitor mechanisms and clinical trials.
Main Results:
- Altered epigenetic patterns, particularly histone modifications, are common in cancer cells.
- HDACs regulate critical cellular functions like transcription, apoptosis, and cell cycle control.
- Dysfunctional HDACs are implicated in cancer, leading to investigation of HDAC inhibitors as therapeutics.
Conclusions:
- HDACs play a significant role in cancer development and progression.
- HDAC inhibitors demonstrate potential as anti-cancer agents through various mechanisms.
- Further research and clinical trials are essential for the therapeutic application of HDAC inhibitors.
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