ArticleACS medicinal chemistry letters2010
Selection, Preparation, and Evaluation of Small- Molecule Inhibitors of Toll-Like Receptor 4.
Article in ACS medicinal chemistry letters, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 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
14 citing papers in PubMed, 28 citations in OpenAlex.
- Inhibition of RNA-binding proteins with small molecules.Nature reviews. Chemistry · 2020Review
- TLR4-dependent fibroblast activation drives persistent organ fibrosis in skin and lung.JCI insight · 2018Article
- Evaluation of TLR4 Inhibitor, T5342126, in Modulation of Ethanol-Drinking Behavior in Alcohol-Dependent Mice.Alcohol and alcoholism (Oxford, Oxfordshire) · 2016Article
- Computational Approaches to Toll-Like Receptor 4 Modulation.Molecules (Basel, Switzerland) · 2016Review
- Pharmacological characterization of the opioid inactive isomers (+)-naltrexone and (+)-naloxone as antagonists of toll-like receptor 4.British journal of pharmacology · 2016Article
- Therapeutic Developments Targeting Toll-like Receptor-4-Mediated Neuroinflammation.ChemMedChem · 2016Review
- Identification of a functional interaction of HMGB1 with Receptor for Advanced Glycation End-products in a model of neuropathic pain.Brain, behavior, and immunity · 2014Article
- Rationally Designed Macrocyclic Peptides as Synergistic Agonists of LPS-Induced Inflammatory Response.Tetrahedron · 2014Article
- Toll-like receptor 4 (TLR4) modulation by synthetic and natural compounds: an update.Journal of medicinal chemistry · 2014Article
- Selection, synthesis, and anti-inflammatory evaluation of the arylidene malonate derivatives as TLR4 signaling inhibitors.Bioorganic & medicinal chemistry · 2012Article
- Neuroexcitatory effects of morphine-3-glucuronide are dependent on Toll-like receptor 4 signaling.Journal of neuroinflammation · 2012Article
- Morphine activates neuroinflammation in a manner parallel to endotoxin.Proceedings of the National Academy of Sciences of the United States of America · 2012Article
- Development of β-amino alcohol derivatives that inhibit Toll-like receptor 4 mediated inflammatory response as potential antiseptics.Journal of medicinal chemistry · 2011Article
- Small-molecule inhibitors of the TLR3/dsRNA complex.Journal of the American Chemical Society · 2011Article
Corrections and comments
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Authors and funding
8 authors at 2 institutions in 1 country.
Funding
Abstract
Toll-like receptor 4 (TLR4), a membrane spanning receptor protein that functions in complex with its accessory protein MD-2, is an intriguing target for therapeutic development. Herein we report the identification of a series of novel TLR4 inhibitors and the development of a robust, enantioselective synthesis using an unprecedented Mannich-type reaction to functionalize a pyrazole ring. In silico and cellular assay results demonstrated that compound 1 and its analogues selectively block TLR4 activation in live cells. Animal model tests showed that 1 and its derivatives could potentiate morphine-induced analgesia in vivo, presumably by attenuating the opioid-induced TLR4 activation.
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.