Nε-Thioacetyl-Lysine-Containing Tri-, Tetra-, and Pentapeptides as SIRT1 and SIRT2 Inhibitors
Nε-Thioacetyl-Lysine-Containing Tri-, Tetra-, and Pentapeptides as SIRT1 and SIRT2 Inhibitors
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DOI：
10.1021/jm801401k
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发表时间：
2009-04-09
影响因子：
7.3
通讯作者：
Jarho, Elina M.
中科院分区：
文献类型：
--
作者：
Kiviranta, Paivi H.;Suuronen, Tiina;Jarho, Elina M.
研究了基于β-微管蛋白和p53蛋白序列的含N-β-硫代乙酰基-赖氨酸的三肽、四肽和五肽作为SIRT 1和SIRT 2抑制剂。五肽的效力取决于侧链的选择。五肽的N-和C-末端残基的去除产生保留SIRT 1抑制活性但降低SIRT 2抑制活性的三肽。最有效的SIRT 1抑制剂与参比化合物（6-氯-2，3，4，9-四氢-1H-咔唑-1-甲酰胺）等效，IC 50值为180-330 nM。
N-epsilon-Thioacetyl-lysine-containing tri-, tetra-, and pentapeptides, based on the (x-tubulin and p53 protein sequences, were studied as SIRT1 and SIRT2 inhibitors. The potency of the pentapeptides depended on the selection of the side chains. The removal of N- and C-terminal residues of the pentapeptides; yielded tripeptides with retained SIRT1 inhibitory activity but decreased SIRT2 inhibitory activity. The most potent SIRT1 inhibitors were equipotent with the reference compound (6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide) with the IC50 values of 180-330 nM.