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Updated: Jan 1, 2026

Assessing Cellular Target Engagement by SHP2 PTPN11 Phosphatase Inhibitors
Published on: July 17, 2020
Targeting SHP2 as a promising strategy for cancer immunotherapy
Qianqian Liu1, Jiao Qu1, Mingxia Zhao1
1State Key Laboratory of Pharmaceutical Biotechnology, Department of Biotechnology and Pharmaceutical Sciences, School of Life Science, Nanjing University, 163 Xianlin Avenue, Nanjing, 210023, China.
Abstract:
Src homology-2-containing protein tyrosine phosphatase 2 (SHP2) is a major phosphatase involved in several cellular processes. In recent years, SHP2 has been the focus of significant attention in human diseases, particular in cancer. Several studies have shown that SHP2 plays an important role in regulating immune cell functions in tumor microenvironment. A few clinical trials conducted using SHP2 allosteric inhibitors have shown remarkable anti-tumor benefits and good safety profiles. This review focuses on the current understanding of the regulation of SHP2 and highlights the vital roles of SHP2 in T lymphocytes, macrophages and cancer cells. It also summarizes the current development of SHP2 inhibitors as a promising strategy for cancer immunotherapy.
Insights
Src homology-2-containing protein tyrosine phosphatase 2 (SHP2) is crucial in cancer and immune responses. SHP2 inhibitors show promise as a cancer immunotherapy strategy.
Area of Science:
- Biochemistry
- Immunology
- Oncology
Background:
- Src homology-2-containing protein tyrosine phosphatase 2 (SHP2) is a key phosphatase regulating cellular functions.
- SHP2 is increasingly recognized for its role in human diseases, especially cancer.
- SHP2 influences immune cell activity within the tumor microenvironment.
Purpose of the Study:
- To review the regulation of SHP2.
- To highlight SHP2's roles in T lymphocytes, macrophages, and cancer cells.
- To summarize the development of SHP2 inhibitors for cancer immunotherapy.
Main Methods:
- Literature review of SHP2 regulation.
- Analysis of SHP2 function in immune cells and cancer.
- Summary of clinical trial data for SHP2 inhibitors.
Main Results:
- SHP2 plays a vital role in T lymphocytes, macrophages, and cancer cells.
- SHP2 allosteric inhibitors have demonstrated significant anti-tumor effects in clinical trials.
- SHP2 inhibitors exhibit favorable safety profiles.
Conclusions:
- SHP2 is a critical target for cancer therapy.
- SHP2 inhibitors represent a promising avenue for cancer immunotherapy development.
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