Issue 10, 2020
From the journal:

Chemical Communications

Protein degradation through covalent inhibitor-based PROTACs†

Gang Xue,a   Jiahui Chen,a   Lihong Liu,a   Danli Zhou,a   Yingying Zuo,a   Tiancheng Fua  and  Zhengying Pan ORCID logo *a  

* Corresponding authors

a State Key Laboratory of Chemical Oncogenomics, Key Laboratory of Chemical Genomics, Engineering Laboratory for Chiral Drug Synthesis, School of Chemical Biology and Biotechnology Shenzhen Graduate School, Peking University, Xili University Town, PKU Campus, F-311, Shenzhen, China
E-mail: panzy@pkusz.edu.cn

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

About
Cited by
Related
Download options Please wait...

Supplementary files

Article information

DOI
https://doi.org/10.1039/C9CC08238G
Article type
Communication
Submitted
21 Oct 2019
Accepted
27 Dec 2019
First published
10 Jan 2020

Chem. Commun., 2020,56, 1521-1524

Permissions

Request permissions

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, 56, 1521 DOI: 10.1039/C9CC08238G

To request permission to reproduce material from this article, please go to the Copyright Clearance Center request page.

If you are an author contributing to an RSC publication, you do not need to request permission provided correct acknowledgement is given.

If you are the author of this article, you do not need to request permission to reproduce figures and diagrams provided correct acknowledgement is given. If you want to reproduce the whole article in a third-party publication (excluding your thesis/dissertation for which permission is not required) please go to the Copyright Clearance Center request page.

Read more about how to correctly acknowledge RSC content.

Social activity

Spotlight

Advertisements