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Updated: Jun 16, 2026

Assessing Cellular Target Engagement by SHP2 (PTPN11) Phosphatase Inhibitors
Published on: July 17, 2020
Recent progress of Src SH2 and SH3 inhibitors as anticancer agents
Xiao-Ling Lu1, Xin Cao, Xiao-Yu Liu
1Department of Biochemistry and Molecular Biology, Second Military Medical University, Shanghai, P.R. China.
Abstract:
Src family tyrosine kinases (SFKs) play key roles in regulating signal transduction in cellular processes. However, hyper-activated SFKs lead to uncontrolled cell proliferation and cancers. For both Src SH2 and SH3 domains involve in the regulation of tumorigenesis signal pathways, the SH2 and SH3 inhibition strategies are expected to block the protein-protein interactions between SFKs and their corporation proteins to abolish the signal transduction. Many inhibitors of SH2 and SH3 domain have been identified. Herein, some predominant examples of these inhibitors are reviewed.
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