ReviewPharmaceuticals (Basel, Switzerland)2022
Therapeutic Targeting of TLR4 for Inflammation, Infection, and Cancer: A Perspective for Disaccharide Lipid A Mimetics.
Review in Pharmaceuticals (Basel, Switzerland), 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 37 papers.
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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
37 citing papers in PubMed, 61 citations in OpenAlex.
- Leuconostoc mesenteroides TH-ST373 Cell-Free Supernatant Against Multidrug-Resistant Escherichia coli.Probiotics and antimicrobial proteins · 2026Article
- Morin ameliorates lipopolysaccharide-induced acute kidney injury in rats via alteration of TLR4/NF-κB, COX-2/PGE2, and monocyte chemoattractant protein-1/CXCL1 signaling pathway.Indian journal of pharmacology · 2026Article
- Identification and evaluation of tumor pyroptosis-associated antigens for design a vaccine candidate against lung cancer.Scientific reports · 2026Article
- Myeloid-derived suppressor cells and their subsets serve as potential biomarkers for the progression of brucellosis.Frontiers in microbiology · 2026Article
- Ginsenoside Rb1-enhanced decellularized extracellular matrix hydrogels ameliorates mitochondrial dysfunction and cellular aging in sepsis-induced acute lung injury.Journal of ginseng research · 2026Article
- The Role of TLR2/TLR4 Receptors in Host Genetic Susceptibility to Recurrent Vulvovaginitis.Journal of fungi (Basel, Switzerland) · 2025Review
- Endotoxin's Impact on Organism: From Immune Activation to Tolerance and Beyond.Journal of clinical medicine · 2025Review
- Biomaterials nanoplatform-based tumor vaccines for immunotherapy.Bioactive materials · 2025Review
- Structural and Immunological Insights into the Lipooligosaccharide of the Marine BacteriumMarine drugs · 2025Article
- Review
- The role of TLR-4 in chemoresistance of cancer.Discover oncology · 2025Review
- Structural insight into TLR4/MD-2 activation by synthetic LPS mimetics with distinct binding modes.Nature communications · 2025Article
- Roles of the gut microbiota in hepatocellular carcinoma: from the gut dysbiosis to the intratumoral microbiota.Cell death discovery · 2025Review
- Deep-Sea-Derived Isobisvertinol Targets TLR4 to Exhibit Neuroprotective Activity via Anti-Inflammatory and Ferroptosis-Inhibitory Effects.Marine drugs · 2025Article
- Adaptive attenuation of virulence mediated by Wzc mutation in ST11-KL47 Carbapenem-resistantFrontiers in cellular and infection microbiology · 2025Article
- Exploring the antioxidant, antiglycation, and anti-inflammatory potential of Oroxylum indicum stem bark extracts.PloS one · 2025Article
- Targeting toll-like receptors: unveiling potential therapeutic strategies for deep vein thrombosis.Frontiers in immunology · 2025Review
- The balance between proinflammatory, "bad", and immunomodulatory, "good", lipopolysaccharide for understanding gut-derived systemic inflammation.Frontiers in immunology · 2025Review
- Adopting orphan receptors: zebrafish Tlr4 homologs mediate responses to group IX/X transition metals.Frontiers in immunology · 2025Article
- Computational Identification and Anti-Inflammatory Evaluation of T19093 as a TLR4/MD2 Inhibitor.Current topics in medicinal chemistry · 2025Article
Corrections and comments
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Authors and funding
2 authors at 2 institutions in 2 countries.
Funding
Abstract
The Toll-like receptor 4 (TLR4) signaling pathway plays a central role in the prompt defense against infectious challenge and provides immediate response to Gram-negative bacterial infection. The TLR4/MD-2 complex can sense and respond to various pathogen-associated molecular patterns (PAMPs) with bacterial lipopolysaccharide (LPS) being the most potent and the most frequently occurring activator of the TLR4-mediated inflammation. TLR4 is believed to be both a friend and foe since improperly regulated TLR4 signaling can result in the overactivation of immune responses leading to sepsis, acute lung injury, or pathologic chronic inflammation involved in cancer and autoimmune disease. TLR4 is also considered a legitimate target for vaccine adjuvant development since its activation can boost the adaptive immune responses. The dual action of the TLR4 complex justifies the efforts in the development of both TLR4 antagonists as antisepsis drug candidates or remedies for chronic inflammatory diseases and TLR4 agonists as vaccine adjuvants or immunotherapeutics. In this review, we provide a brief overview of the biochemical evidences for possible pharmacologic applications of TLR4 ligands as therapeutics and report our systematic studies on the design, synthesis, and immunobiological evaluation of carbohydrate-based TLR4 antagonists with nanomolar affinity for MD-2 as well as disaccharide-based TLR4 agonists with picomolar affinity for the TLR4/MD-2 complex.
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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.