The Current State of NAD<sup>+</sup>‐Dependent Histone Deacetylases (Sirtuins) as Novel Therapeutic Targets
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- Matthias Schiedel
- Institute of Pharmaceutical Sciences Albert‐Ludwigs‐Universität Freiburg Freiburg Germany
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- Dina Robaa
- Department of Pharmaceutical Chemistry Martin‐Luther Universität Halle‐Wittenberg Halle/Saale Germany
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- Tobias Rumpf
- Institute of Pharmaceutical Sciences Albert‐Ludwigs‐Universität Freiburg Freiburg Germany
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- Wolfgang Sippl
- Department of Pharmaceutical Chemistry Martin‐Luther Universität Halle‐Wittenberg Halle/Saale Germany
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- Manfred Jung
- Institute of Pharmaceutical Sciences Albert‐Ludwigs‐Universität Freiburg Freiburg Germany
抄録
<jats:title>Abstract</jats:title><jats:p>Sirtuins are NAD<jats:sup>+</jats:sup>‐dependent protein deacylases that cleave off acetyl, as well as other acyl groups, from the ε‐amino group of lysines in histones and other substrate proteins. Seven sirtuin isotypes (Sirt1–7) have been identified in mammalian cells. As sirtuins are involved in the regulation of various physiological processes such as cell survival, cell cycle progression, apoptosis, DNA repair, cell metabolism, and caloric restriction, a dysregulation of their enzymatic activity has been associated with the pathogenesis of neoplastic, metabolic, infectious, and neurodegenerative diseases. Thus, sirtuins are promising targets for pharmaceutical intervention. Growing interest in a modulation of sirtuin activity has prompted the discovery of several small molecules, able to inhibit or activate certain sirtuin isotypes. Herein, we give an update to our previous review on the topic in this journal (Schemies, 2010), focusing on recent developments in sirtuin biology, sirtuin modulators, and their potential as novel therapeutic agents.</jats:p>
収録刊行物
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- Medicinal Research Reviews
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Medicinal Research Reviews 38 (1), 147-200, 2017-01-17
Wiley
