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Published on: February 27, 2016
Sirtuin modulators: an updated patent review (2012 - 2014)
Paolo Mellini1, Sergio Valente, Antonello Mai
1Sapienza Università di Roma, Dipartimento di Chimica e Tecnologie del Farmaco , P.le A. Moro 5, 00185 Rome , Italy.
Introduction:
Since 2000 sirtuins (SIRT1-7) have gained growing attention for their connections with many biological processes such as cellular metabolism regulation, neuroprotection, apoptosis, inflammation, and cancer progression. In particular, SIRT1 has been the most studied isoform, not only for its role during caloric restriction but also as target in prevention of aging-related diseases. SIRT inhibition can be useful for treating cancer, HIV infection or muscular diseases, SIRT activation can exert positive effects in aging-related disorders such as metabolism, cardiovascular, and neurodegenerative diseases.
Areas Covered:
This review includes the patents about sirtuin modulation released during the 2012 - 2014 period, and covers the potential therapeutic uses of known sirtuin modulators as well as new related small molecules in various disease contexts.
Expert Opinion:
The effective role of sirtuins in cancer is still controversial, because some of them seem to have tumor-promoter as well as tumor-suppressor properties. Thus, few patents describing SIRT inhibitors have been found in 2012 - 2014 period. Despite the still active debate on their role as direct or indirect activators of SIRT1, sirtuin-activating compounds are actually subjected to intense research for the ability to treat neurodegenerative diseases, metabolic disorders, inflammation, vascular system injuries, wound healing and endothelial dysfunctions. A great number of clinical trials are reported with either SIRT inhibitors or activators, thus it is possible that in the foreseeable future one or more of them will enter in the clinical arena.
Insights
Sirtuin research shows potential for treating aging-related diseases and neurodegeneration. While sirtuin inhibitors are explored for cancer, activators are key for metabolic and inflammatory disorders, with clinical trials underway.
Area of Science:
- Biochemistry
- Molecular Biology
- Pharmacology
Background:
- Sirtuins (SIRT1-7) are crucial regulators of cellular metabolism, neuroprotection, apoptosis, inflammation, and cancer.
- SIRT1 is a key target for aging-related diseases and caloric restriction.
- SIRT modulation offers therapeutic potential for cancer, HIV, muscular diseases, and aging disorders.
Purpose of the Study:
- To review patents on sirtuin modulation from 2012-2014.
- To cover therapeutic applications of known and novel sirtuin modulators.
- To explore sirtuin's role in various disease contexts.
Main Methods:
- Patent literature review (2012-2014).
- Analysis of sirtuin modulators and their therapeutic potential.
- Examination of small molecules targeting sirtuin pathways.
Main Results:
- Sirtuin's role in cancer remains controversial, with both tumor-promoter and suppressor properties observed.
- Few SIRT inhibitors were patented between 2012-2014.
- Sirtuin activators are under intense research for neurodegenerative diseases, metabolic disorders, and inflammation.
Conclusions:
- Sirtuin activators show promise for treating neurodegenerative, metabolic, and inflammatory conditions.
- Ongoing clinical trials for SIRT inhibitors and activators suggest future therapeutic applications.
- Further research is needed to clarify sirtuin's complex role in disease.
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