摘要
SIRT 1是一种烟酰胺腺苷二核苷酸(NAD)依赖的去乙酰化酶,它从多种靶蛋白(如组蛋白、转录因子和辅助因子)中去除乙酰基。SIRT 1催化的这些因素的脱乙酰作用调节下游蛋白的活性,从而影响许多生物过程。SIRT 1参与代谢、炎症和肿瘤生长的调控。这种酶的活性与限制热量有益健康有关,如延长寿命,尤其是SIRT 1的激活对心血管系统有积极的影响。因此,SIRT 1被认为是一种有吸引力的药物靶点,SIRT 1的调控可能是一种新的治疗心血管疾病的策略,因为能够激活SIRT 1的小分子可以被认为是一种心脏保护剂。本文综述了天然化合物和合成化合物作为SIRT 1激活剂的研究进展,重点介绍了它们在心血管疾病治疗中的应用前景。
关键词: SIRT 1,激活剂,STACS,心脏保护,NAD,去乙酰化。
Current Medicinal Chemistry
Title:Activators of Sirtuin-1 and their Involvement in Cardioprotection
Volume: 25 Issue: 34
关键词: SIRT 1,激活剂,STACS,心脏保护,NAD,去乙酰化。
摘要: SIRT1 is a nicotinamide adenosine dinucleotide (NAD+)-dependent deacetylase, which removes acetyl groups from many target proteins, such as histone proteins, transcription factors and cofactors. SIRT1-catalyzed deacetylation of these factors modulates the activity of downstream proteins, thus influencing many biological processes. SIRT1 is involved in the regulation of metabolism, inflammation, and tumor growth. The activity of this enzyme is related to the beneficial health effects of calorie restriction, such as lifespan extension and, in particular, the activation of SIRT1 has a positive impact on the cardiovascular system. Therefore, SIRT1 is considered as an attractive drug target and modulation of SIRT1 may represent a new therapeutic strategy against cardiovascular diseases, as small molecules able to activate SIRT1 can be considered as cardioprotective agents. In this review, we summarize both natural and synthetic compounds developed as SIRT1 activators, with a focus on their promising therapeutic applications in cardiovascular pathologies.
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Activators of Sirtuin-1 and their Involvement in Cardioprotection, Current Medicinal Chemistry 2018; 25 (34) . https://dx.doi.org/10.2174/0929867325666180214115438
DOI https://dx.doi.org/10.2174/0929867325666180214115438 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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