Sirtuins are NAD(+)-dependent protein lysine deacylase and mono-ADP ribosylases present in both prokaryotes and eukaryotes. The sirtuin family comprises seven isoforms in mammals, each possessing different subcellular localization and biological functions. Sirtuins have received increasing attention in the past two decades given their pivotal functions in a variety of biological contexts, including cytodifferentiation, transcriptional regulation, cell cycle progression, apoptosis, inflammation, metabolism, neurological and cardiovascular physiology and cancer. Consequently, modulation of sirtuin activity has been regarded as a promising therapeutic option for many pathologies. In this review, we provide an up-to-date overview of sirtuin biology and pharmacology. We examine the main features of the most relevant inhibitors and activators, analyzing their structure-activity relationships, applications in biology, and therapeutic potential.

Sirtuin modulators: past, present, and future perspectives / Fiorentino, Francesco; Mautone, Nicola; Menna, Martina; D'Acunzo, Francesca; Mai, Antonello; Rotili, Dante. - In: FUTURE MEDICINAL CHEMISTRY. - ISSN 1756-8919. - (2022). [10.4155/fmc-2022-0031]

Sirtuin modulators: past, present, and future perspectives

Fiorentino, Francesco
Primo
;
Mautone, Nicola;Menna, Martina;Mai, Antonello;Rotili, Dante
2022

Abstract

Sirtuins are NAD(+)-dependent protein lysine deacylase and mono-ADP ribosylases present in both prokaryotes and eukaryotes. The sirtuin family comprises seven isoforms in mammals, each possessing different subcellular localization and biological functions. Sirtuins have received increasing attention in the past two decades given their pivotal functions in a variety of biological contexts, including cytodifferentiation, transcriptional regulation, cell cycle progression, apoptosis, inflammation, metabolism, neurological and cardiovascular physiology and cancer. Consequently, modulation of sirtuin activity has been regarded as a promising therapeutic option for many pathologies. In this review, we provide an up-to-date overview of sirtuin biology and pharmacology. We examine the main features of the most relevant inhibitors and activators, analyzing their structure-activity relationships, applications in biology, and therapeutic potential.
aging; cancer; drug discovery; epigenetics; metabolism; neurodegeneration; protein lysine deacylation; sirtuin modulators; sirtuins
01 Pubblicazione su rivista::01d Recensione
Sirtuin modulators: past, present, and future perspectives / Fiorentino, Francesco; Mautone, Nicola; Menna, Martina; D'Acunzo, Francesca; Mai, Antonello; Rotili, Dante. - In: FUTURE MEDICINAL CHEMISTRY. - ISSN 1756-8919. - (2022). [10.4155/fmc-2022-0031]
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11573/1638052
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