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July 31, 2024Journal of Medicinal Chemistry

Discovery of an Exceptionally Orally Bioavailable and Potent HPK1 PROTAC with Enhancement of Antitumor Efficacy of Anti-PD-L1 Therapy

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Abstract

HPK1, a well-known negative regulator of T cell receptors, can cause T cell dysfunction when abnormally activated. In this study, a PROTAC

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Cite This Study

Wu et al. (2024) studied this question.

synapsesocial.com/papers/68e5e3dfb6db643587577ec8 https://doi.org/10.1021/acs.jmedchem.4c00644

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Also Consider

Synapse has enriched 5 closely related papers on similar clinical questions. Consider them for comparative context:

1Discovery of a Novel Potent and Orally Efficacious PROTAC Degrader of HPK1 for Tumor Immunotherapy2025 · 7 citations
2Abstract 4514: Discovery of potent and orally bioavailable degraders of HPK1 based on a novel HPK1 binder2024
3Discovery of Novel HPK1 Inhibitors via Chemistry-Based Direct-to-Bioassay Screening and SAR OptimizationOriginal Research · 2026 · 1 citations
4Discovery of GNE-6893, a Potent, Selective, Orally Bioavailable Small Molecule Inhibitor of HPK12024 · 15 citations
5Abstract 6510: BPI-511966,a potent and selective HPK1 inhibitor with robust single-agent efficacy for cancer immunotherapy2024 · 1 citations