含N(ε)-硫代乙酰赖氨酸的人源SIRT3三肽抑制剂。
Human SIRT3 tripeptidic inhibitors containing N(ε)-thioacetyl-lysine.
作者信息
Chen Bing, Wang Juan, Huang Yajun, Zheng Weiping
机构信息
School of Pharmacy, Jiangsu University, 301 Xuefu Road, Zhenjiang 212013, Jiangsu Province, PR China.
School of Pharmacy, Jiangsu University, 301 Xuefu Road, Zhenjiang 212013, Jiangsu Province, PR China.
出版信息
Bioorg Med Chem Lett. 2015 Sep 1;25(17):3481-7. doi: 10.1016/j.bmcl.2015.07.008. Epub 2015 Jul 10.
Built upon our lead pan-SIRT1/2/3 tripeptidic inhibitors that contain the catalytic mechanism-based sirtuin inhibitory warhead N(ε)-thioacetyl-lysine, three of their analogs (i.e., 7, 9, and 19) were discovered in the current study to exhibit a significantly enhanced SIRT3 inhibitory selectivity while maintaining the SIRT3 inhibitory potency. These compounds represent novel lead compounds for developing more potent and selective SIRT3 inhibitors of the catalytic mechanism-based type.
基于我们领先的泛SIRT1/2/3三肽抑制剂，其含有基于催化机制的sirtuin抑制弹头N(ε)-硫代乙酰赖氨酸，在本研究中发现它们的三个类似物（即7、9和19）在保持SIRT3抑制效力的同时，表现出显著增强的SIRT3抑制选择性。这些化合物代表了用于开发更有效和选择性更高的基于催化机制类型的SIRT3抑制剂的新型先导化合物。
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