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Related Concept Videos

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The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against...
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Related Experiment Video

Updated: Sep 30, 2025

Assessing Cellular Target Engagement by SHP2 PTPN11 Phosphatase Inhibitors
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Proteolysis-targeting chimera molecules targeting SHP2.

Dandan Yu1, Mengzhu Zheng1, Yang Liu2

  • 1Hubei 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.

Future Medicinal Chemistry
|March 17, 2022
PubMed
Summary

SHP2 protein, a target in cancer therapy, can be degraded using Proteolysis-targeting chimera (PROTAC) technology. This review covers existing SHP2 PROTACs and inhibitors, exploring dual PROTACs for treating SHP2-related diseases.

Keywords:
PROTACSHP2SHP2 PROTACSHP2 inhibitordual PROTAC

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Area of Science:

  • Biochemistry
  • Molecular Biology
  • Oncology

Background:

  • SHP2 (encoded by PTPN11) is a non-receptor protein tyrosine phosphatase implicated in oncogenesis.
  • The link between SHP2 and cancer makes it a significant therapeutic target.
  • Proteolysis-targeting chimera (PROTAC) technology offers advantages over traditional inhibitors by inducing protein degradation.

Purpose of the Study:

  • To review reported PROTAC molecules targeting SHP2.
  • To summarize recent SHP2 inhibitors as potential leads for PROTAC development.
  • To introduce dual PROTAC technology for SHP2-related diseases.

Main Methods:

  • Literature review of published SHP2 PROTACs.
  • Summary of recently reported SHP2 inhibitors.
  • Discussion of dual PROTAC technology principles.

Main Results:

  • Four PROTAC molecules targeting SHP2 have been reported.
  • SHP2 inhibitors identified can serve as starting points for new PROTAC designs.
  • Dual PROTAC technology presents a novel approach for treating SHP2-driven diseases.

Conclusions:

  • PROTAC technology is a promising strategy for targeting SHP2 in cancer.
  • Further development of SHP2 PROTACs is warranted.
  • Dual PROTACs may offer an alternative to combination therapies for SHP2-related cancers.