ArticleACS medicinal chemistry letters2023
Discovery of First-in-Class Small Molecule Inhibitors of Lymphocyte Activation Gene 3 (LAG-3).
Article in ACS medicinal chemistry letters, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
19 citing papers in PubMed, 31 citations in OpenAlex.
- LAG3 checkpoint function and its mechanism of action in therapeutic targeting.Nature reviews. Immunology · 2026Review
- HTS-Oracle X: AI-Guided Prospective Discovery of Small Molecule Immune Checkpoint Binders.ACS medicinal chemistry letters · 2026Article
- 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
- Study on the Molecular Dynamics of 2‑(4-Fluorophenyl)-6-methyl-4-(3- (trifluoromethyl)phenyl)-1,2-dihydrodipyrazolo[3,4-b:3',4'‑ACS omega · 2025Article
- Phenotypic and targeted drug discovery in immune therapeutics: challenges, opportunities, and future directions.RSC advances · 2025Review
- Exploring new frontiers in LAG-3 biology and therapeutics.Trends in pharmacological sciences · 2025Review
- Negative Immune Checkpoint Inhibitors.Pharmaceutics · 2025Review
- LAG Time in the Era of Immunotherapy-New Molecular Insights Into the Immunosuppression Mechanism of Lymphocyte Activation Gene-3.Immunological reviews · 2025Review
- Zebularine showed anti-tumor efficacy in clear cell renal cell carcinoma.Frontiers in pharmacology · 2025Article
- Discovery of ICOS-Targeted Small Molecules Using Affinity Selection Mass Spectrometry Screening.ChemMedChem · 2024Article
- From Virtual Screens to Cellular Target Engagement: New Small Molecule Ligands for the Immune Checkpoint LAG-3.ACS medicinal chemistry letters · 2024Article
- Small molecules from antibody pharmacophores (SMAbPs) as a hit identification workflow for immune checkpoints.Science advances · 2024Article
- Deciphering LAG-3: unveiling molecular mechanisms and clinical advancements.Biomarker research · 2024Review
- Discovery of ICOS-targeted small molecules using affinity selection mass spectrometry screening.bioRxiv : the preprint server for biology · 2024Article
- ImmunoPET imaging of LAG-3 expression in tumor microenvironment withJournal for immunotherapy of cancer · 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
- Lymphocyte-activation gene 3 in cancer immunotherapy: function, prognostic biomarker and therapeutic potentials.Frontiers in immunology · 2024Review
Corrections and comments
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Authors and funding
3 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Lymphocyte activation gene 3 (LAG-3) is a negative immune checkpoint that plays a key role in downregulating the immune response to cancer. Inhibition of LAG-3 interactions allows T cells to regain cytotoxic activity and reduce the immunosuppressive function of regulating T cells. We utilized a combination approach of focused screening and "SAR by catalog" to identify small molecules that function as dual inhibitors of the interactions of LAG-3 with major histocompatibility complex (MHC) class II and fibrinogen-like protein 1 (FGL1). Our top hit compound inhibited both LAG-3/MHCII and LAG-3/FGL1 interactions in biochemical binding assays with IC
Identifiers
What OpenQuestion holds
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.