ArticleEuropean journal of clinical pharmacology2020
Effect of chemical modulation of toll-like receptor 4 in an animal model of ulcerative colitis.
Article in European journal of clinical pharmacology, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Who cites it
12 citing papers in PubMed, 18 citations in OpenAlex.
- Qijiao Shengbai capsule ameliorates ulcerative colitis in mice by modulating gut microbiota and protecting the intestinal barrier, associated with suppression of the TLR4/MyD88/NF-κB pathway.Frontiers in microbiology · 2026Article
- Gentiopicroside improves DSS-induced ulcerative colitis and secondary liver injury in mice by enhancing the intestinal barrier and regulating the gut microbiome.Scientific reports · 2025Article
- AhR governs lipid metabolism: the role of gut microbiota.Frontiers in microbiology · 2025Review
- Resatorvid (TAK-242) Ameliorates Ulcerative Colitis by Modulating Macrophage Polarization and T Helper Cell Balance via TLR4/JAK2/STAT3 Signaling Pathway.Inflammation · 2024Article
- Alterations in macrophage polarization in the craniofacial and extracranial skeleton after zoledronate application and surgical interventions - anFrontiers in immunology · 2023Article
- Synthetic Glycolipids as Molecular Vaccine Adjuvants: Mechanism of Action in Human Cells and In Vivo Activity.Journal of medicinal chemistry · 2021Article
- Synthetic glycolipid-based TLR4 antagonists negatively regulate TRIF-dependent TLR4 signalling in human macrophages.Innate immunity · 2021Article
- Palmitoylethanolamide Modulation of Microglia Activation: Characterization of Mechanisms of Action and Implication for Its Neuroprotective Effects.International journal of molecular sciences · 2021Article
- Toll-like receptor 4 (TLR4) antagonists as potential therapeutics for intestinal inflammation.Indian journal of gastroenterology : official journal of the Indian Society of Gastroenterology · 2021Review
- Article
- Synthesis, Molecular Modeling and Biological Evaluation of Metabolically Stable Analogues of the Endogenous Fatty Acid Amide Palmitoylethanolamide.International journal of molecular sciences · 2020Article
- Preclinical development of the TLR4 antagonist FP12 as a drug lead targeting the HMGB1/MD-2/TLR4 axis in lethal influenza infection.Innate immunityArticle
Corrections and comments
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Authors and funding
9 authors at 2 institutions in 1 country.
Funding
Abstract
purposeThe partial ineffectiveness and side effects of inflammatory bowel disease (IBD) current therapies drive basic research to look for new therapeutic target in order to develop new drug lead. Considering the pivotal role played by toll-like receptors (TLRs) in gut inflammation, we evaluate here the therapeutic effect of the synthetic glycolipid TLR4 antagonist FP7.
methodsThe anti-inflammatory effect of FP7, active as TLR4 antagonist, was evaluated on peripheral blood mononuclear cells (PBMCs) and lamina propria mononuclear cells (LPMCs) isolated from IBD patients, and in a mouse model of ulcerative colitis.
resultsFP7 strongly reduced the inflammatory responses induced by lipopolysaccharide (LPS) in vitro, due to its capacity to compete with LPS for the binding of TLR4/MD-2 receptor complex thus inhibiting both the MyD88- and TRIF-dependent inflammatory pathways. Colitic mice treated with FP7 exhibit reduced colonic inflammation and decreased levels of pro-inflammatory cytokines.
conclusionsThis study suggests that TLR4 chemical modulation can be an effective therapeutic approach to IBD. The selectivity of FP7 on TLR4 makes this molecule a promising drug lead for new small molecules-based treatments.
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