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Emerging Therapeutic Potential of SIRT6 Modulators
Francesco Fiorentino1, Antonello Mai2, Dante Rotili2
1Department of Chemistry, University of Oxford, South Parks Road, Oxford OX1 3QZ, United Kingdom.
Journal of Medicinal Chemistry
|July 2, 2021
Summary
Sirtuin 6 (SIRT6) is a key enzyme in cellular health, DNA repair, and aging. Researchers are developing small molecules to activate or inhibit SIRT6 for treating diseases like cancer and age-related disorders.
Area of Science:
- Biochemistry
- Molecular Biology
- Pharmacology
Background:
- Sirtuin 6 (SIRT6) is an NAD+-dependent enzyme with diverse roles in DNA repair, metabolism, and aging.
- SIRT6 exhibits context-dependent functions in cancer, acting as both a tumor suppressor and promoter.
- Its critical role in cellular homeostasis makes SIRT6 a significant therapeutic target.
Purpose of the Study:
- To review the current understanding of SIRT6 pharmacology and medicinal chemistry.
- To describe the characteristics of identified SIRT6 activators and inhibitors.
- To highlight SIRT6 as a promising target for therapeutic interventions.
Main Methods:
- Literature review of in vitro and in vivo studies on SIRT6.
- Analysis of identified small-molecule SIRT6 modulators (activators and inhibitors).
- Discussion of the pharmacological relevance and medicinal chemistry of SIRT6.
Main Results:
- SIRT6 modulation impacts DNA repair, metabolic regulation, and aging processes.
- Small molecules targeting SIRT6 have been identified, offering therapeutic potential.
- These modulators aid in scrutinizing SIRT6 activity and validating its pharmacological role.
Conclusions:
- SIRT6 is a versatile enzyme with significant implications in health and disease.
- Pharmacological targeting of SIRT6 holds promise for treating cancer and age-related conditions.
- Further research into SIRT6 modulators can advance therapeutic strategies.
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