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Assessing Cellular Target Engagement by SHP2 PTPN11 Phosphatase Inhibitors
Published on: July 17, 2020
Little ones can do big things: Small molecule inhibitors target PTPN2/PTPN1 for tumor immunotherapy
Junyu Wang1, Shugang Qin2, Anren Zhang1
1Department of Rehabilitation Medicine Shanghai Fourth People's Hospital, School of Medicine, Tongji University Shanghai China.
Abstract:
AC484 was developed by designing compounds based on the PTPN2 protein structure. AC484 enhances antitumor immunity through multiple mechanisms: increasing tumor sensitivity to IFN-γ, improving T-cell functions, stimulating tumor microenvironment inflammation, expanding TCR diversity, and preventing T-cell exhaustion. Interestingly, the efficacy of AC484 was also mediated by CD8+ and NK cells.
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