Issue 72, 2022
From the journal:

Chemical Communications

Reactive oxygen species-responsive Pre-PROTAC for tumor-specific protein degradation†

Haixia Liu,‡ab   Chaowei Ren,‡ac   Renhong Sun,a   Huihui Wang,ac   Yuexiong Zhan,a   Xiaobao Yang,*ad   Biao Jiang*abce  and  Hongli Chen ORCID logo *a  

* Corresponding authors

a Shanghai Institute for Advanced Immunochemical Studies, ShanghaiTech University, 393 Middle Huaxia Road, Pudong, Shanghai, China
E-mail: chenhl@shanghaitech.edu.cn, jiang-biao@shanghaitech.edu.cn, yang.xiaobao@gluetacs.com

b School of Physical Science and Technology, ShanghaiTech University, 393 Middle Huaxia Road, Pudong, Shanghai, China

c School of Life Science and Technology, ShanghaiTech University, 393 Middle Huaxia Road, Pudong, Shanghai, China

d Gluetacs Therapeutics (Shanghai) Co., Ltd., 99 Haike Road, Zhangjiang Hi-Tech Park, Shanghai, China

e CAS Key Laboratory of Synthetic Chemistry of Natural Substances, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, 345 Lingling Road, Shanghai 200032, China

Abstract

By introducing a reactive oxygen species (ROS) triggered leaving group (arylboronic acid) to the parent PROTACs, ROS-responsive Pre-PROTACs were designed and evaluated. Pre-PROTAC (7) efficiently degraded the target protein BRD3 according to ROS levels. Our research provides an effective approach to control PROTAC activation by the endogenous ROS-related microenvironment.

Graphical abstract: Reactive oxygen species-responsive Pre-PROTAC for tumor-specific protein degradation

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Article information

DOI
https://doi.org/10.1039/D2CC03367D
Article type
Communication
Submitted
16 Jun 2022
Accepted
12 Aug 2022
First published
12 Aug 2022

Chem. Commun., 2022,58, 10072-10075

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Reactive oxygen species-responsive Pre-PROTAC for tumor-specific protein degradation

H. Liu, C. Ren, R. Sun, H. Wang, Y. Zhan, X. Yang, B. Jiang and H. Chen, Chem. Commun., 2022, 58, 10072 DOI: 10.1039/D2CC03367D

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