ArticleRSC medicinal chemistry2023
First-in-class small molecule inhibitors of ICOS/ICOSL interaction as a novel class of immunomodulators.
Article in RSC medicinal chemistry, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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The trial behind it
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Who cites it
13 citing papers in PubMed.
- HTS-Oracle X: AI-Guided Prospective Discovery of Small Molecule Immune Checkpoint Binders.ACS medicinal chemistry letters · 2026Article
- Article
- Discovery of CD28-Targeted Small Molecule Inhibitors of T Cell Co-Stimulation Using Affinity Selection-Mass Spectrometry (AS-MS) and Ex Vivo Validation.Journal of medicinal chemistry · 2025Article
- CD28 and ICOS in immune regulation: Structural insights and therapeutic targeting.Bioorganic & medicinal chemistry letters · 2025Review
- Phenotypic and targeted drug discovery in immune therapeutics: challenges, opportunities, and future directions.RSC advances · 2025Review
- Computational Design of a Bicyclic Peptide Inhibitor Targeting the ICOS/ICOS-L Protein-Protein Interaction.Chemical biology & drug design · 2025Article
- Enhanced ICOS Signaling Between Dendritic Cells and T Cells Characterizes the Immune Landscape of Human Cholangiocarcinoma.Human mutation · 2025Article
- Discovery of ICOS-Targeted Small Molecules Using Affinity Selection Mass Spectrometry Screening.ChemMedChem · 2024Article
- Small molecules from antibody pharmacophores (SMAbPs) as a hit identification workflow for immune checkpoints.Science advances · 2024Article
- Discovery of ICOS-targeted small molecules using affinity selection mass spectrometry screening.bioRxiv : the preprint server for biology · 2024Article
- Structure-Based Rational Design of Constrained Peptides as TIM-3 Inhibitors.ACS medicinal chemistry letters · 2024Article
- Review
- Inhibitors of Immune Checkpoints: Small Molecule- and Peptide-Based Approaches.Journal of personalized medicine · 2024Review
Corrections and comments
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Authors and funding
3 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The interaction of the inducible co-stimulator (ICOS) with its ligand (ICOSL) plays key roles in T-cell differentiation and activation of T-cell to B-cell functions. The ICOS/ICOSL pathway is a validated target for T-cell lymphomas induced by the proliferation of T-follicular helper (Tfh) cells. Moreover, the inhibition of ICOS/ICOSL interaction can decrease the enhancement of immunosuppressive regulatory T cells (Tregs) in both hematologic malignancies and solid tumors. However, targeting ICOS/ICOSL interaction is currently restricted to monoclonal antibodies (mAbs) and there are no small molecules in existence that can block ICOS/ICOSL. To fill this gap, we report herein the first time-resolved fluorescence resonance energy transfer (TR-FRET) assay to evaluate the ability of small molecules to inhibit ICOS/ICOSL interaction. Implementation of the developed TR-FRET assay in high-throughput screening (HTS) of a focused chemical library resulted in the identification of
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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 OpenQuestion graph.