Sirtuin activators and inhibitors: Promises, achievements, and challenges.
Sirtuin activators and inhibitors: Promises, achievements, and challenges.
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DOI：
10.1016/j.pharmthera.2018.03.004
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发表时间：
2018-08
影响因子：
13.5
通讯作者：
Steegborn C
中科院分区：
文献类型：
--
作者：
Dai H;Sinclair DA;Ellis JL;Steegborn C
Sirtuin家族的NAD+依赖的蛋白赖氨酸脱酰酶调节从能量代谢到应激反应的各种生理功能。人类Sirtuin亚型SIRT1-7被认为是治疗与衰老相关的疾病的有吸引力的靶点，如2型糖尿病、炎症性疾病和神经退行性疾病。我们回顾了Sirtuin靶向药物发现和开发的现状。已经有了有效的和选择性的药理Sirt1激活剂和抑制剂，并进行了初步的临床试验。几种有希望的抑制剂和激活剂也被描述为其他异构体。这类化合物对Sirtuin调控机制的研究进展为进一步的药物开发提供了合理的基础。
The NAD+-dependent protein lysine deacylases of the Sirtuin family regulate various physiological functions, from energy metabolism to stress responses. The human Sirtuin isoforms, SIRT1-7, are considered attractive therapeutic targets for aging-related diseases, such as type 2 diabetes, inflammatory diseases and neurodegenerative disorders. We review the status of Sirtuin-targeted drug discovery and development. Potent and selective pharmacological Sirt1 activators and inhibitors are available, and initial clinical trials have been carried out. Several promising inhibitors and activators have also been described for other isoforms. Progress in understanding the mechanisms of Sirtuin modulation by such compounds provides a rational basis for further drug development.
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影响因子：
29
作者：
Chalkiadaki A;Guarente L
通讯作者：
Guarente L
影响因子：
4.8
作者：
Balan, Vitaly;Miller, Gregory S.;Tzivion, Guri
通讯作者：
Tzivion, Guri
影响因子：
2.7
作者：
Bemis, Jean E.;Vu, Chi B.;Perni, Robert B.
通讯作者：
Perni, Robert B.
影响因子：
7.3
作者：
Disch, Jeremy S.;Evindar, Ghotas;Perni, Robert B.
通讯作者：
Perni, Robert B.
影响因子：
29
作者：
Banks AS;Kon N;Knight C;Matsumoto M;Gutiérrez-Juárez R;Rossetti L;Gu W;Accili D
通讯作者：
Accili D