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Updated: Jul 19, 2025

Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
Recent histone deacetylase inhibitors in cancer therapy
Roza Parveen1, Divya Harihar2, Biswa Prasun Chatterji3
1Faculty of Medicine and Health Sciences, Tampere University, Tampere, Finland.
Abstract:
Cancer metastasis increases the complexity of the disease and escalates patient mortality. Traditional chemotherapy has been associated with low efficacy and marked side effects. Studies pivot toward histone deacetylase (HDAC) enzymes and inhibitors because they are critical for chromatin structure, gene regulation, and cellular activities that are linked to metastasis and cancer progression. HDAC inhibitors (HDACi) can alter gene expression patterns and can lead to cell-cycle arrest and apoptosis in neoplastic cells. Several HDACi drugs like vorinostat, romidepsin, panobinostat, and belinostat are approved by the Food and Drug Administration. China and Japan have approved the use of tucidinostat, a new subtype-selective HDACi that inhibits class 1 HDAC1, HDAC2, HDAC3, as well as class 2b HDAC10. These drugs have shown promising results in the treatment of multiple carcinoma including cervical cancer, T-cell lymphoma, brain cancer, and breast cancer. This review highlights the HDACi classes, the mechanism of action of these inhibitors, their preclinical and clinical efficacy, and the latest clinical trials and patents used in cancer therapeutics. Overall, this review focuses on patents and clinical trials data from 2019 onward to give a better viewpoint on current trends in HDACis as chemotherapy agents.
Insights
Histone deacetylase inhibitors (HDACi) show promise in cancer treatment by targeting metastasis and gene regulation. Recent clinical trials and patents from 2019 onward highlight their evolving role as effective chemotherapy agents.
Area of Science:
- Oncology
- Molecular Biology
- Pharmacology
Background:
- Cancer metastasis significantly increases mortality, with traditional chemotherapy often exhibiting limited efficacy and severe side effects.
- Histone deacetylase (HDAC) enzymes are crucial for chromatin structure and gene regulation, playing a key role in cancer progression and metastasis.
- HDAC inhibitors (HDACi) offer a therapeutic strategy by modulating gene expression, inducing cell-cycle arrest, and promoting apoptosis in cancer cells.
Purpose of the Study:
- To review the current landscape of HDAC inhibitors in cancer therapeutics.
- To highlight recent clinical trials and patents (2019 onwards) related to HDACi.
- To provide an overview of HDACi classes, mechanisms of action, and efficacy in various cancers.
Main Methods:
- Literature review focusing on HDAC inhibitors in cancer therapy.
- Analysis of preclinical and clinical efficacy data.
- Examination of recent patents and clinical trial data from 2019 to present.
Main Results:
- Several HDACi drugs (e.g., vorinostat, tucidinostat) are approved and show efficacy in various cancers like cervical cancer, lymphoma, and breast cancer.
- Subtype-selective HDACi, such as tucidinostat, target specific HDAC classes (1, 2, 3, 10) with promising results.
- Recent data from 2019 onward indicates ongoing research and development in HDACi for cancer treatment.
Conclusions:
- HDAC inhibitors represent a significant advancement in cancer therapy, offering improved efficacy and targeted mechanisms.
- The continued investigation of HDACi through clinical trials and patent filings underscores their potential as next-generation chemotherapy agents.
- HDACi demonstrate broad applicability across multiple cancer types, highlighting their therapeutic versatility.
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