Related Experiment Videos
Sirtuin Inhibition: Strategies, Inhibitors, and Therapeutic Potential
Yanhong Jiang1, Jiajia Liu1, Di Chen1
1School of Pharmacy, Jiangsu University, 301 Xuefu Road, Zhenjiang 212013, Jiangsu Province, PR China.
Abstract:
The β-NAD+-dependent Nε-acyl-lysine deacylation reaction catalyzed by sirtuin family members has been increasingly demonstrated to be important in regulating multiple crucial cellular processes and has also been proposed to be a therapeutic target for multiple human diseases. Accordingly, its inhibitors have been actively pursued over the past few years. In addition, we have also seen the pharmacological assessment of sirtuin inhibitory compounds, although to a lesser extent. In this review, we first discuss how sirtuin inhibitors were discovered with the use of various approaches. We then follow with a discussion of pharmacological studies using sirtuin inhibitors. Our aim here is to set a stage for developing future superior sirtuin inhibitors and for an expanded effort in exploiting inhibitors to explore and/or validate the therapeutic potential stemming from the inhibition of the sirtuin-catalyzed deacylation reaction.
Insights
Sirtuin inhibitors, crucial for cellular processes and disease treatment, are actively pursued. This review details their discovery and pharmacological use, aiming to guide future development for therapeutic applications.
Area of Science:
- Biochemistry
- Molecular Biology
- Pharmacology
Background:
- Sirtuins catalyze β-NAD+-dependent deacylation reactions.
- These reactions regulate critical cellular processes.
- Sirtuin inhibition is a therapeutic target for human diseases.
Purpose of the Study:
- To review methods for discovering sirtuin inhibitors.
- To discuss pharmacological studies of sirtuin inhibitors.
- To guide the development of superior sirtuin inhibitors and explore their therapeutic potential.
Main Methods:
- Literature review of sirtuin inhibitor discovery approaches.
- Analysis of pharmacological studies involving sirtuin inhibitors.
Main Results:
- Various approaches have been employed for sirtuin inhibitor discovery.
- Pharmacological assessments of sirtuin inhibitors have been conducted.
Conclusions:
- Understanding inhibitor discovery and pharmacology is key.
- Future efforts should focus on developing superior inhibitors.
- Exploiting sirtuin inhibition offers therapeutic potential for diseases.