An activity-based probe developed by a sequential dehydroalanine formation strategy targets HECT E3 ubiquitin ligases
An activity-based probe developed by a sequential dehydroalanine formation strategy targets HECT E3 ubiquitin ligases
复制标题
通过连续脱氢丙氨酸形成策略开发的基于活性的探针，针对 HECT E3 泛素连接酶
DOI：
10.1039/c9cc03739j
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发表时间：
2019
影响因子：
4.9
通讯作者：
Shi Jing
中科院分区：
文献类型：
--
作者：
Xu Ling;Fan Jian;Wang Yu;Zhang Zhongping;Fu Yao;Li Yi-Ming;Shi Jing
E3 ligases play a critical role in ubiquitin (Ub) conjugation cascades, and any aberration in their activity is associated with a number of diseases. Advancement in our knowledge of understanding the roles of HECT E3s requires biochemical tools such as activity-based probes (ABPs). In this study we developed a novel dehydroalanine (Dha)-based E2-Ub ABP using a strategy that is a combination of practical hydrazide-based native chemical ligation and sequential Dha formation. The probe could be used for labeling HECT E3s not only in vitro but also in endogenous cellular contexts. Our easy-to-implement method is expected to be useful for the preparation of Dha based Ub family E2 conjugate ABPs.
