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Updated: Dec 29, 2025

Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
Histone deacetylase (HDAC) inhibitors in cancer: a patent review (2017-present)
Chunlong Zhao1, Hang Dong1, Qifu Xu1
1Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, Ji'nan, China.
Abstract:
Introduction: Histone deacetylase (HDAC) inhibitors play a crucial role in restoring the balance of acetylation and deacetylation of lysine residues of histones and non-histone proteins, which are applied to treat several diseases including cancer.Area covered: This review covers recent efforts in the synthesis and applications of inhibitors and hybrid inhibitors targeting HDAC from 2017 to 2019.Expert opinion: HDACs are important epigenetic targets and HDAC inhibitors have become important biologically active compounds for the treatment of cancers. Among the recent patents available, most of them place emphasis on HDAC selective inhibitors and multitarget HDAC inhibitors. Although great accomplishments have been achieved in developing HDAC selective inhibitors, there is still an urgent need for discovery of novel HDAC inhibitors with new zinc-binding groups avoiding the unfavorable pharmacokinetics profiles of hydroxamic acid. Apart from cancer therapy, HDAC inhibitors have recently been considered as a new strategy in treating other human diseases, such as alcohol use disorder (AUD), neurological disorders, age-related diseases, and so forth.
Insights
Histone deacetylase (HDAC) inhibitors are vital for treating cancers by regulating protein acetylation. Recent research focuses on novel HDAC inhibitors for improved cancer therapy and other diseases.
Area of Science:
- Epigenetics
- Medicinal Chemistry
- Pharmacology
Background:
- Histone deacetylase (HDAC) inhibitors are critical for managing acetylation/deacetylation balance in histones and non-histone proteins.
- HDACs represent significant epigenetic targets, with their inhibitors being key compounds in cancer treatment.
- Recent advancements focus on selective and multitarget HDAC inhibitors.
Purpose of the Study:
- To review recent advancements in the synthesis and application of HDAC inhibitors and hybrid inhibitors.
- To highlight the progress and challenges in developing novel HDAC inhibitors.
- To explore emerging therapeutic applications of HDAC inhibitors beyond cancer.
Main Methods:
- Literature review of scientific publications and patents from 2017-2019.
- Analysis of synthetic strategies for novel HDAC inhibitors.
- Evaluation of therapeutic applications and pharmacokinetic profiles.
Main Results:
- Significant progress in developing selective and multitarget HDAC inhibitors.
- Identification of a need for novel zinc-binding groups to overcome pharmacokinetic limitations of hydroxamic acids.
- Exploration of HDAC inhibitors for treating alcohol use disorder, neurological disorders, and age-related diseases.
Conclusions:
- HDAC inhibitors are crucial in cancer therapy and show promise for other diseases.
- Development of novel HDAC inhibitors with improved pharmacokinetic profiles is essential.
- Continued research into HDAC inhibitors offers new therapeutic strategies for various human conditions.
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