Proteolysis-targeting chimera molecules targeting SHP2

Author:

Yu Dandan1,Zheng Mengzhu1,Liu Yang2,Chen Lixia2ORCID,Li Hua12ORCID

Affiliation:

1. Hubei Key Laboratory of Natural Medicinal Chemistry & Resource Evaluation, School of Pharmacy, Tongji-Rongcheng Center for Biomedicine, Tongji Medical College, Huazhong University of Science & Technology, Wuhan, 430030, China

2. Wuya College of Innovation, Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang, 110016, China

Abstract

SHP2 is a member of the non-receptor protein tyrosine phosphatases, encoded by PTPN11, and exhibits oncogenic activities. The close association between SHP2 and human cancer has made SHP2 a promising target for clinical therapy. Proteolysis-targeting chimera (PROTAC) technology utilizes the degradation mechanism of the ubiquitin proteasome system to degrade specific proteins. It has strong advantages compared with inhibitors. Here we list the four reported PROTAC molecules targeting SHP2 and summarize the recently reported SHP2 inhibitors which can provide lead compounds for designing new SHP2 PROTACs. We also introduce the dual PROTAC technology which may replace drug combinations to treat SHP2-related diseases.

Funder

The Liaoning Revitalization Talents Program

The Liaoning Province Natural Science Foundation

National Natural Science Foundation of China

The National Megaproject for Innovative Drugs

The Chunhui Program-Cooperative Research Project of the Ministry of Education

Publisher

Future Science Ltd

Subject

Drug Discovery,Pharmacology,Molecular Medicine

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