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Updated: Apr 5, 2026

Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
Selective Histone Deacetylase Inhibitors with Anticancer Activity
1Institute of Traditional Chinese Medicine & Natural Products, College of Pharmacy, Jinan University, Guangzhou 510632, P.R. China. chyewc@gmail.com.
Abstract:
HDAC inhibitors (HDACIs), which can be used to kill cancer cells through inhibiting histone deacetylase activity or altering the structure of chromatin, have emerged as efficacious agents in the treatment of cancer. With SAHA, FK228, belinostat and panobinostat approved by the FDA, displaying satisfying activity in both haematological and solid tumors of various tissues, efforts to create selective HDACIs have been attracted attention over the past several years. Herein, we mainly review the progress of selective HDAC inhibitors including class-selective and isoform-selective HDAC inhibitors.
Insights
Histone deacetylase inhibitors (HDACIs) are effective cancer treatments. This review focuses on the development of selective HDACIs, including class-selective and isoform-selective inhibitors, for improved cancer therapy.
Area of Science:
- Oncology
- Molecular Biology
- Pharmacology
Background:
- Histone deacetylase inhibitors (HDACIs) demonstrate efficacy in cancer treatment by modulating histone deacetylase activity and chromatin structure.
- Several HDACIs, including SAHA, FK228, belinostat, and panobinostat, are FDA-approved and show activity in both hematological and solid tumors.
Purpose of the Study:
- To review the advancements in the development of selective HDAC inhibitors.
- To highlight progress in both class-selective and isoform-selective HDAC inhibitors.
Main Methods:
- Literature review of scientific publications and clinical trial data.
- Analysis of research trends in selective HDAC inhibitor development.
Main Results:
- Significant progress has been made in designing HDACIs with improved selectivity.
- Selective HDAC inhibitors offer potential for targeted cancer therapy with reduced side effects.
Conclusions:
- The development of selective HDAC inhibitors is a key area of focus in cancer drug discovery.
- Further research into class- and isoform-selective HDACIs holds promise for next-generation cancer treatments.
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