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Protein degradation through covalent inhibitor-based PROTACs

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Abstract

Tremendous advancements in proteolysis targeting chimera (PROTAC) technology have been made in recent years. However, whether a covalent inhibitor-based PROTAC can be developed remains controversial. Here, we successfully developed chimeric degraders based on covalent inhibitors to degrade BTK and BLK kinases, demonstrating that covalent inhibitor-based PROTACs are viable and useful tools.

Graphical abstract: Protein degradation through covalent inhibitor-based PROTACs

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Article information


Submitted
21 Oct 2019
Accepted
27 Dec 2019
First published
10 Jan 2020

Chem. Commun., 2020, Advance Article
Article type
Communication

Protein degradation through covalent inhibitor-based PROTACs

G. Xue, J. Chen, L. Liu, D. Zhou, Y. Zuo, T. Fu and Z. Pan, Chem. Commun., 2020, Advance Article , DOI: 10.1039/C9CC08238G

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