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Cyclic tripeptide-based potent human SIRT7 inhibitors
Shengchao Li1, Bo Wu1, Weiping Zheng1
1School of Pharmacy, Jiangsu University, 301 Xuefu Road, Zhenjiang 212013, Jiangsu Province, PR China.
Bioorganic & Medicinal Chemistry Letters
|December 23, 2018
Summary
Researchers identified potent inhibitors for human SIRT7 deacetylase activity. These cyclic tripeptides, featuring unique catalytic warheads, offer a breakthrough for developing targeted SIRT7 therapies.
Area of Science:
- Biochemistry
- Molecular Biology
- Medicinal Chemistry
Background:
- Sirtuins are a class of NAD+-dependent deacetylases involved in various cellular processes.
- Human SIRT7 (sirtuin 7) is implicated in ribosome biogenesis and cancer, making it a therapeutic target.
- Potent and selective inhibitors for SIRT7 are currently lacking.
Purpose of the Study:
- To identify novel inhibitors targeting the deacetylase activity of human SIRT7.
- To explore the potential of cyclic tripeptides with specific catalytic warheads as SIRT7 inhibitors.
Main Methods:
- Synthesis of two cyclic tripeptides incorporating thiourea-type and carboxamide-type catalytic mechanism-based inhibitory warheads.
- Biochemical assays to evaluate the inhibitory potency against purified human SIRT7 deacetylase activity.
- Assessment of cross-reactivity against other human sirtuin isoforms (SIRT1, SIRT2, SIRT3, SIRT6).
Main Results:
- Two novel cyclic tripeptides demonstrated potent inhibition of human SIRT7 deacetylase activity at low micromolar concentrations.
- These compounds exhibited broad inhibitory activity across five tested human sirtuins (SIRT1/2/3/6/7).
- This study reports the first identification of potent SIRT7 inhibitors.
Conclusions:
- The identified cyclic tripeptides are the first potent inhibitors discovered for human SIRT7.
- These findings provide a foundation for developing more selective and potent SIRT7-targeting therapeutics.
- Further research can optimize these compounds for enhanced specificity and therapeutic applications.
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