ArticleCell chemical biology2018
Small-Molecule TLR8 Antagonists via Structure-Based Rational Design.
Article in Cell chemical biology, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 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.
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Who cites it
21 citing papers in PubMed, 56 citations in OpenAlex.
- TLR8 Stimulation Leads to Microenvironment Activation and Enhanced Antibody-Dependent Cellular Responses in CLL.International journal of molecular sciences · 2026Article
- Synthetic viral RNA mimetics induce neuronal loss through microglial phagocytosis.Inflammation research : official journal of the European Histamine Research Society ... [et al.] · 2026Article
- Targeting pattern recognition receptors for cancer therapy: Mechanisms and strategies.Acta pharmaceutica Sinica. B · 2025Review
- Discovery of Potent and Selective Quinoline-Based Toll-like Receptor 9 Antagonists.ACS medicinal chemistry letters · 2025Article
- Damage-associated molecular patterns (DAMPs) in diseases: implications for therapy.Molecular biomedicine · 2025Review
- Discovery of Novel Isoxazole-Based Small-Molecule Toll-Like Receptor 8 Antagonists.Journal of medicinal chemistry · 2025Article
- Label-free biosensor assay decodes the dynamics of Toll-like receptor signaling.Nature communications · 2024Article
- Targeting toll-like receptor 7 as a therapeutic development strategy for systemic lupus erythematosus.Acta pharmaceutica Sinica. B · 2024Article
- 4-Aminoquinoline as a privileged scaffold for the design of leishmanicidal agents: structure-property relationships and key biological targets.Frontiers in chemistry · 2024Review
- Modulation of IRAK enzymes as a therapeutic strategy against SARS-CoV-2 induced cytokine storm.Clinical and experimental medicine · 2023Review
- Next-Generation Adjuvants: Applying Engineering Methods to Create and Evaluate Novel Immunological Responses.Pharmaceutics · 2023Article
- Integrated approaches for the recognition of small molecule inhibitors for Toll-like receptor 4.Computational and structural biotechnology journal · 2023Article
- Protocol for evaluation and validation of TLR8 antagonists in HEK-Blue cells via secreted embryonic alkaline phosphatase assay.STAR protocols · 2022Article
- HIV-1 Tat endocytosis and retention in endolysosomes affects HIV-1 Tat-induced LTR transactivation in astrocytes.FASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2022Article
- Activation of Innate Immunity by Therapeutic Nucleic Acids.International journal of molecular sciences · 2021Review
- Tetrasubstituted imidazoles as incognito Toll-like receptor 8 a(nta)gonists.Nature communications · 2021Article
- Structural and functional understanding of the toll-like receptors.Protein science : a publication of the Protein Society · 2021Review
- Targeting the innate immune receptor TLR8 using small-molecule agents.Acta crystallographica. Section D, Structural biology · 2020Review
- Sensing of HIV-1 by TLR8 activates human T cells and reverses latency.Nature communications · 2020Article
- The Bacterial Product Violacein Exerts an Immunostimulatory Effect Via TLR8.Scientific reports · 2019Article
Corrections and comments
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Authors and funding
11 authors at 4 institutions in 3 countries.
Funding
Abstract
Rational design of drug-like small-molecule ligands based on structural information of proteins remains a significant challenge in chemical biology. In particular, designs targeting protein-protein interfaces have met little success given the dynamic nature of the protein surfaces. Herein, we utilized the structure of a small-molecule ligand in complex with Toll-like receptor 8 (TLR8) as a model system due to TLR8's clinical relevance. Overactivation of TLR8 has been suggested to play a prominent role in the pathogenesis of various autoimmune diseases; however, there are still few small-molecule antagonists available, and our rational designs led to the discovery of six exceptionally potent compounds with ∼picomolar IC
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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.