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Issue 49, 2019
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An activity-based probe developed by a sequential dehydroalanine formation strategy targets HECT E3 ubiquitin ligases

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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

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Supplementary files

Article information


Submitted
15 May 2019
Accepted
23 May 2019
First published
24 May 2019

Chem. Commun., 2019,55, 7109-7112
Article type
Communication

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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