Articlenpj drug discovery2024
Synthesis and characterization of soquelitinib a selective ITK inhibitor that modulates tumor immunity.
Article in npj drug discovery, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
What it found
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
8 citing papers in PubMed.
- Atopic Dermatitis: New Targets and Emerging Systemic Therapies.American journal of clinical dermatology · 2026Review
- Phosphotyrosine proteomics reveals novel Zap70 and Itk pathway targets downstream of TCR and CAR in Jurkat T cells.Scientific reports · 2026Article
- Discovery of an ITK and TRK kinase inhibitor for the potential topical treatment of atopic dermatitis.Nature communications · 2026Article
- ITK-targeted immune remodeling enhanced the efficacy of anti-CD19 CAR-T cell therapy.Cell death discovery · 2026Article
- Phosphoproteomic analysis of successive Jurkat CD19-CAR generations reveals TCRζ-driven signalling.Cellular signalling · 2026Article
- Fibroblast TGF-β signaling defines spatial tumor ecosystems linked to immune checkpoint blockade resistance.Communications biology · 2025Article
- Targeting Intracellular Pathways in Atopic Dermatitis with Small Molecule Therapeutics.Current issues in molecular biology · 2025Review
- Advancements in research on the cardiovascular toxicity caused by TEC family kinases inhibitors.Frontiers in pharmacology · 2025Review
Corrections and comments
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Authors and funding
16 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
ITK is a kinase involved in T cell activation, proliferation and differentiation. In mice, selective knock-out of the ITK gene produces Th1 skewing of T helper cell differentiation. Soquelitinib, a covalent ITK inhibitor, blocks ITK activity with greater than 100-fold selectivity compared to inhibition of a related kinase, RLK. We describe the chemistry and biologic effects of soquelitinib. In vitro studies with normal or malignant T cells demonstrated that soquelitinib suppresses Th2 cytokine production preferentially with relative sparing of Th1 cytokines. Soquelitinib inhibits the in vivo growth of several syngeneic murine tumors including those that do not express ITK. Treatment with soquelitinib leads to increased tumor infiltration of normal CD8+ cells that possess enhanced T effector function. Soquelitinib reduced expression of T cell exhaustion markers and was able to restore T effector function to exhausted cells. Pharmacologic selective ITK inhibition may represent a novel approach to cancer immunotherapy.
Identifiers
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Registered trials
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.