一种基于机制的强效组蛋白去乙酰化酶抑制剂，包含 Nε-硫代碳酰胺赖氨酸（TuAcK）。
A mechanism-based potent sirtuin inhibitor containing Nε-thiocarbamoyl-lysine (TuAcK).
机构信息
Department of Chemistry, University of Akron, Akron, OH 44325, USA.
出版信息
Bioorg Med Chem Lett. 2011 Aug 15;21(16):4753-7. doi: 10.1016/j.bmcl.2011.06.069. Epub 2011 Jun 22.
Abstract
In the current study, we have identified N(ε)-thiocarbamoyl-lysine (TuAcK) as a general sirtuin inhibitory warhead which was shown to be able to confer potent sirtuin inhibition. This inhibition was also shown to be mechanism-based in that the TuAck residue was able to be processed by a sirtuin enzyme with the formation of a stalled S-alkylamidate intermediate.
摘要
在当前的研究中，我们已经确定 N(ε)-硫代碳酰胺赖氨酸（TuAcK）为一种通用的组蛋白去乙酰化酶抑制弹头，它被证明能够赋予强烈的组蛋白去乙酰化酶抑制作用。这种抑制作用也被证明是基于机制的，因为 TuAck 残基能够被组蛋白去乙酰化酶酶促加工，形成一个停滞的 S-烷基酰胺中间产物。
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