ArticleNature communications2023
A small molecule inhibitor of PTP1B and PTPN2 enhances T cell anti-tumor immunity.
Article in Nature communications, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 46 papers.
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Who cites it
46 citing papers in PubMed.
- Ptpn2 limits plasma cell fate and antiviral immunity by integrating B cell receptor and IFN-γ signals in B cells.Science advances · 2026Article
- Molecular Mechanisms and Targeted Therapies of PTPN2 in Metabolic Diseases: A Review.Biomolecules · 2026Review
- Pentacyclic triterpenoids fromRSC advances · 2026Article
- PTPN1/PTPN2 inhibition improves NK cancer therapy by enhancing IL-2 and mitigating TGFβ1 responses.EMBO reports · 2026Article
- Dual immunosuppression mechanism induced by PTP1B in colorectal cancer: upregulation of PD-L1 by FOXO1/miR-34C/c-MYC axis and inhibition of the infiltration of CD8(+) T cell by downregulating of CXCL11.Journal of translational medicine · 2026Article
- Multi-omics identification of a programmed cell death-related signature and potential target P4HB for bladder cancer based on a 101-combination machine learning and experimental validation.Clinical and experimental medicine · 2026Article
- An integrated approach for novel PTP1B inhibitor screening: combining machine learning models, molecular docking, molecular and dynamics simulations.Molecular diversity · 2026Article
- Investigation into the Anti-hyperglycemic Traits and Bioactive Constituents of Postbiotics Derived from Lacticaseibacillus paracasei NCUH012072.Probiotics and antimicrobial proteins · 2026Article
- Mechanisms, functions and therapeutic targeting of protein tyrosine phosphatases.Nature reviews. Molecular cell biology · 2026Review
- Organoplatinum(II) Type II Immunogenic Cell Death Inducers Target Protein Tyrosine Phosphatase 1B to Drive Immunogenicity.Journal of the American Chemical Society · 2026Article
- False Friends in Fluorescence - Simple HPLC Evaluation of False Positive Fragment Hits in a DiFMUP Assay for Protein Tyrosine Phosphatase 1B.Drug design, development and therapy · 2026Article
- Mapping of PTP1B, TCPTP, SHP2, and Putative Substrates Reveals Novel Networks in Glomerular Podocytes.Journal of cellular physiology · 2026Article
- HIT101308137 and HIT104293658 nominate dual target chemotypes for PTPN1 and PTPN2 with preliminary selectivity in colorectal cancer cells.Frontiers in chemistry · 2026Article
- Supercharging the metabolic engine: mitochondrial engineering strategies for CAR-T persistence in solid tumors.Frontiers in immunology · 2026Review
- Identification of novel PTP1B inhibitor for the treatment of LPS-induced myocardial apoptosis: machine learning based virtual screening and biological evaluation.Journal of enzyme inhibition and medicinal chemistry · 2025Article
- Disentangling Metabolite Detection from Pathway Stress Using Biosensors.ACS synthetic biology · 2025Article
- Uncovering the individual immunotherapeutic roles of PTPN1 and PTPN2 in T cells during dual inhibition.iScience · 2025Article
- Activatable PROTAC nanoassembly for photodynamic PTP1B proteolysis enhances glioblastoma immunotherapy.Acta pharmaceutica Sinica. B · 2025Article
- Adjusting the scope of natural killer cells in cancer therapy.Cellular & molecular immunology · 2025Review
- Multicatalysis-Enabled Multicomponent Reactions Generate a PTP1B Inhibitor.ACS central science · 2025Article
Corrections and comments
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Authors and funding
14 authors.
Funding
Abstract
The inhibition of protein tyrosine phosphatases 1B (PTP1B) and N2 (PTPN2) has emerged as an exciting approach for bolstering T cell anti-tumor immunity. ABBV-CLS-484 is a PTP1B/PTPN2 inhibitor in clinical trials for solid tumors. Here we have explored the therapeutic potential of a related small-molecule-inhibitor, Compound-182. We demonstrate that Compound-182 is a highly potent and selective active site competitive inhibitor of PTP1B and PTPN2 that enhances T cell recruitment and activation and represses the growth of tumors in mice, without promoting overt immune-related toxicities. The enhanced anti-tumor immunity in immunogenic tumors can be ascribed to the inhibition of PTP1B/PTPN2 in T cells, whereas in cold tumors, Compound-182 elicited direct effects on both tumor cells and T cells. Importantly, treatment with Compound-182 rendered otherwise resistant tumors sensitive to α-PD-1 therapy. Our findings establish the potential for small molecule inhibitors of PTP1B and PTPN2 to enhance anti-tumor immunity and combat cancer.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the Socratic graph.