Nε-thioacetyl-lysine:: A multi-facet functional probe for enzymatic protein lysine Nε-deacetylation

被引：93

作者：

Fatkins, David G. ^{[1
]}

Monnot, Andrew D. ^{[1
]}

Zheng, Weiping ^{[1
]}

机构：

[1] Univ Akron, Dept Chem, Akron, OH 44325 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 14期

关键词：

N-epsilon-acetyl-lysine; N-epsilon-thioacetyl-lysine; protein deacetylases;

D O I：

10.1016/j.bmcl.2006.04.075

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Peptides containing N-epsilon-thioacetyl-lysine and N-epsilon-acetyl-lysine were evaluated for their de(thio)acetylation catalyzed by human HDAC8 and SIRT1, two distinct protein deacetylases. N epsilon-Thioacetyl-lysine was found to be a mimic of N epsilon-acetyl-lysine for HDAC8-catalyzed reaction, but to confer inhibition against SIRT1. These results point to further diverse applications based on NE-thioacetyl-lysine. (c) 2006 Elsevier Ltd. All rights reserved.

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收藏

页码：3651 / 3656

页数：6

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