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Sirtuin modulators: where are we now? A review of patents from 2015 to 2019
Nicola Mautone1, Clemens Zwergel1,2, Antonello Mai1
1Dipartimento di Chimica e Tecnologie del Farmaco, "Sapienza" Università di Roma, Rome, Italy.
Abstract:
In recent years, sirtuins (SIRTs) gained an increasing consideration because of their multiple key roles in several biological settings such as the regulation of transcription, energetic metabolism, cell cycle progression, and cytodifferentiation, apoptosis, neuro- and cardio-protection, inflammation, cancer onset and progression. Since there is mounting evidence in favor of potential therapeutic applications of SIRT modulators in various age-related disorders, the search about them is quite active. Areas covered: This review includes the patents regarding SIRT modulators released from 2015 to 2019 and provides an overview of the most relevant SIRT modulators.Expert opinion: Despite the knowledge about this family of broad-spectrum protein lysine deacylases has recently massively increased, there are still open questions, first of all, the exact nature of their involvement in various age-related conditions. The search for isoform-specific SIRT activators and inhibitors is still at its infancy, a limited number of patents describing them has been released, and not many clinical trials are ongoing. However, it is extremely likely that the successes obtained in the structural elucidation and structure-based design approaches that very recently have led to potent and specific SIRT modulators will pave the way for the development of further compounds selective for every single isoform.
Insights
Sirtuins (SIRTs) are key regulators in many biological processes. Research into SIRT modulators for age-related diseases is active, with recent advances in developing specific modulators.
Area of Science:
- Biochemistry
- Pharmacology
- Molecular Biology
Background:
- Sirtuins (SIRTs) play critical roles in transcription, metabolism, cell cycle, differentiation, apoptosis, neuroprotection, cardioprotection, inflammation, and cancer.
- Growing evidence suggests therapeutic potential for SIRT modulators in age-related disorders, driving active research.
- This review focuses on patents and modulators from 2015-2019.
Purpose of the Study:
- To review patents concerning SIRT modulators from 2015 to 2019.
- To provide an overview of significant SIRT modulators identified during this period.
- To discuss the current state and future directions of SIRT modulator research.
Main Methods:
- Patent literature search for SIRT modulators (2015-2019).
- Analysis and categorization of identified SIRT modulators.
- Review of existing knowledge on sirtuin functions and therapeutic applications.
Main Results:
- A significant number of patents related to SIRT modulators were released between 2015 and 2019.
- Several relevant SIRT modulators have been identified and characterized.
- The development of potent and specific SIRT modulators has been advanced by structural and design approaches.
Conclusions:
- Despite increased knowledge, the precise role of SIRTs in age-related conditions requires further elucidation.
- Research into isoform-specific SIRT activators and inhibitors is nascent, with limited clinical trials.
- Advances in structural biology and rational drug design are expected to yield more selective SIRT modulators for therapeutic development.
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