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Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
Histone deacetylase inhibitors: new hope for rheumatoid arthritis?
1Department of Pharmacy National University of Singapore 10 Kent Ridge Crescent Singapore 119260.
Abstract:
Histone deacetylase (HDAC) inhibitors are a new family of anti-cancer agents currently undergoing clinical investigations for various oncology indications. Their anti-inflammatory activities had been well documented and they appear to be potential therapeutic strategies for various inflammatory diseases. In this review, the anti-inflammatory activities of HDAC inhibitors with emphasis on their potential applications in rheumatoid arthritis (RA) will be summarized. The possible anti-rheumatic mechanisms, including growth arrest in rheumatoid arthritis synovial fibroblasts (RASFs), suppression of pro-inflammatory cytokines or chemokines, anti-angiogenesis as well as protective effects on bone and cartilage destruction will also be discussed. Current literatures strongly imply HDAC inhibitors as innovative anti-rheumatic drug candidates. However, long-term safety is a major concern. Future investigations should focus on identification of molecular anti-rheumatic mechanisms, development of new classes of HDAC inhibitors with better safety and selectivity profiles, combination of HDAC inhibitors with disease modifying anti-rheumatic drugs (DMARDs) and establishment of topical or intra-articular formulations.
Insights
Histone deacetylase (HDAC) inhibitors show promise for treating inflammatory diseases like rheumatoid arthritis (RA). Further research is needed to improve their safety and efficacy for long-term use.
Area of Science:
- Pharmacology
- Immunology
- Rheumatology
Background:
- Histone deacetylase (HDAC) inhibitors are emerging anti-cancer agents.
- HDAC inhibitors possess documented anti-inflammatory properties, suggesting therapeutic potential for inflammatory diseases.
Purpose of the Study:
- To review the anti-inflammatory activities of HDAC inhibitors.
- To summarize their potential applications in rheumatoid arthritis (RA).
Main Methods:
- Review of current literature on HDAC inhibitors and their anti-inflammatory effects.
- Discussion of potential anti-rheumatic mechanisms.
Main Results:
- HDAC inhibitors demonstrate potential anti-rheumatic mechanisms, including inhibiting rheumatoid arthritis synovial fibroblast (RASF) growth, suppressing pro-inflammatory cytokines/chemokines, and reducing angiogenesis.
- Evidence suggests protective effects against bone and cartilage destruction in RA.
Conclusions:
- HDAC inhibitors represent promising candidates for novel anti-rheumatic therapies.
- Long-term safety remains a significant concern requiring further investigation.
- Future research should focus on elucidating molecular mechanisms, developing safer and more selective inhibitors, exploring combination therapies with disease-modifying anti-rheumatic drugs (DMARDs), and developing targeted formulations.
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