ArticleACS chemical biology2018
A High Content Screen in Macrophages Identifies Small Molecule Modulators of STING-IRF3 and NFkB Signaling.
Article in ACS chemical biology, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
What it found
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The trial behind it
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Who cites it
12 citing papers in PubMed, 27 citations in OpenAlex.
- Identification of drug candidates against glioblastoma with machine learning and high-throughput screening of heterogeneous cellular models.Digital discovery · 2026Article
- A dual-fluorescence assay for gene delivery vehicle screening in macrophages with an inflammation-inducible reporter construct.BMC methods · 2025Article
- Mechanisms underlying the compromised clinical efficacy of interferon in clearing HBV.Virology journal · 2024Review
- High-Content Image-Based Screening and Deep Learning for the Detection of Anti-Inflammatory Drug Leads.Chembiochem : a European journal of chemical biology · 2024Article
- High-Content Screening and Computational Prediction Reveal Viral Genes That Suppress the Innate Immune Response.mSystems · 2022Article
- Molecular Dynamics Simulations Reveal the Modulated Mechanism of STING Conformation.Interdisciplinary sciences, computational life sciences · 2021Article
- From Phenotypic Hit to Chemical Probe: Chemical Biology Approaches to Elucidate Small Molecule Action in Complex Biological Systems.Molecules (Basel, Switzerland) · 2020Review
- Molecular design, synthesis and biological characterization of novel Resveratrol derivative as potential anticancer agent targeting NF-κB.Journal of applied biomedicine · 2020Article
- MGL1 Receptor Plays a Key Role in the Control ofCells · 2020Article
- Interrupting cyclic dinucleotide-cGAS-STING axis with small molecules.MedChemComm · 2019Review
- Discovery of a Novel cGAMP Competitive Ligand of the Inactive Form of STING.ACS medicinal chemistry letters · 2019Article
- Screening for new macrophage therapeutics.Theranostics · 2019Review
Corrections and comments
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Authors and funding
10 authors at 1 institution in 1 country.
Funding
Abstract
We screened a library of bioactive small molecules for activators and inhibitors of innate immune signaling through IRF3 and NFkB pathways with the goals of advancing pathway understanding and discovering probes for immunology research. We used high content screening to measure the translocation from the cytoplasm to nucleus of IRF3 and NFkB in primary human macrophages; these transcription factors play a critical role in the activation of STING and other pro-inflammatory pathways. Our pathway activator screen yielded a diverse set of hits that promoted nuclear translocation of IRF3 and/or NFkB, but the majority of these compounds did not cause activation of downstream pathways. Screening for antagonists of the STING pathway yielded multiple kinase inhibitors, some of which inhibit kinases not previously known to regulate the activity of this pathway. Structure-activity relationships (SARs) and subsequent chemical proteomics experiments suggested that MAPKAPK5 (PRAK) is a kinase that regulates IRF3 translocation in human macrophages. Our work establishes a high content screening approach for measuring pro-inflammatory pathways in human macrophages and identifies novel ways to inhibit such pathways; among the targets of the screen are several molecules that may merit further development as anti-inflammatory drugs.
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Registered trials
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