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基于脱氢丙氨酸的双泛素化活性探针。

Dehydroalanine-based diubiquitin activity probes.

机构信息

Department of Chemistry, Ben-Gurion University of the Negev , Beer Sheva 84105, Israel.

出版信息

Org Lett. 2014 Jan 17;16(2):540-3. doi: 10.1021/ol403416w. Epub 2013 Dec 24.

Abstract

A strategy for the synthesis of dehydroalanine based diubiquitin activity probes is described. The site-specific introduction of dehydroalanine was achieved from diubiquitin bearing Cys residue near the scissile bond between two ubiquitins linked through Lys48, Lys63 or in a head to tail fashion. The probes were characterized for their activities with various deubiquitinases, which open new opportunities in studying deubiquitinases in various settings.

摘要

本文描述了一种基于脱氢丙氨酸的双泛素活性探针的合成策略。通过在靠近两个泛素之间的裂解键的二泛素上带有 Cys 残基的位置特异性引入脱氢丙氨酸,实现了通过 Lys48、Lys63 或从头至尾的方式连接的二泛素。这些探针的活性特征与各种去泛素化酶进行了表征,这为在各种环境中研究去泛素化酶开辟了新的机会。

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