Issue 49, 2019

An activity-based probe developed by a sequential dehydroalanine formation strategy targets HECT E3 ubiquitin ligases

Abstract

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.

Graphical abstract: An activity-based probe developed by a sequential dehydroalanine formation strategy targets HECT E3 ubiquitin ligases

Supplementary files

Article information

Article type
Communication
Submitted
15 May 2019
Accepted
23 May 2019
First published
24 May 2019

Chem. Commun., 2019,55, 7109-7112

An activity-based probe developed by a sequential dehydroalanine formation strategy targets HECT E3 ubiquitin ligases

L. Xu, J. Fan, Y. Wang, Z. Zhang, Y. Fu, Y. Li and J. Shi, Chem. Commun., 2019, 55, 7109 DOI: 10.1039/C9CC03739J

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