ArticleThe Journal of biological chemistry2014
A novel small-molecule tumor necrosis factor α inhibitor attenuates inflammation in a hepatitis mouse model.
Article in The Journal of biological chemistry, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 26 papers.
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Who cites it
26 citing papers in PubMed, 66 citations in OpenAlex.
- Peptide-Based Regulation of TNF-α-Mediated Cytotoxicity.Biomolecules · 2025Article
- Emodin mitigates rheumatoid arthritis through direct binding to TNF-α.Frontiers in pharmacology · 2025Article
- CTRP13-Mediated Effects on Endothelial Cell Function and Their Potential Role in Obesity.Cells · 2024Article
- The Exacerbating Effects of the Tumor Necrosis Factor in Cardiovascular Stenosis: Intimal Hyperplasia.Cancers · 2024Review
- Cooperative NF-κB and Notch1 signaling promotes macrophage-mediated MenaINV expression in breast cancer.Breast cancer research : BCR · 2023Article
- Biosensor-based active ingredient recognition system for screening TNF-α inhibitors from lotus leaves.Analytical and bioanalytical chemistry · 2023Article
- A Small Molecule Selected from a DNA-Encoded Library of Natural Products That Binds to TNF-α and Attenuates Inflammation In Vivo.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2022Article
- The anti-inflammatory effects of apigenin and genistein on the rat intestinal epithelial (IEC-6) cells with TNF-α stimulation in response to heat treatment.Current research in food science · 2022Article
- A Novel Competitive Binding Screening Assay Reveals Sennoside B as a Potent Natural Product Inhibitor of TNF-α.Biomedicines · 2021Article
- Tumor Necrosis Factor Alpha-Mediated Inflammation and Remodeling of the Extracellular Matrix Underlies Aortic Stiffening Induced by the Common Chemotherapeutic Agent Doxorubicin.Hypertension (Dallas, Tex. : 1979) · 2021Article
- TNFα promotes oral cancer growth, pain, and Schwann cell activation.Scientific reports · 2021Article
- A Rational Insight into the Effect of Dimethyl Sulfoxide on TNF-α Activity.International journal of molecular sciences · 2020Article
- Noncompetitive Allosteric Antagonism of Death Receptor 5 by a Synthetic Affibody Ligand.Biochemistry · 2020Article
- TNFα inhibitor C87 sensitizes EGFRvIII transfected glioblastoma cells to gefitinib by a concurrent blockade of TNFα signaling.Cancer biology & medicine · 2019Article
- Overexpression of the C-domain of angiotensin-converting enzyme reduces melanoma growth by stimulating M1 macrophage polarization.The Journal of biological chemistry · 2019Article
- Incorporation of macrophages into engineered skeletal muscle enables enhanced muscle regeneration.Nature biomedical engineering · 2018Article
- A New Venue of TNF Targeting.International journal of molecular sciences · 2018Review
- Design, Synthesis, and Evaluation of Dihydrobenzo[Frontiers in chemistry · 2018Article
- TNF Receptor Type II as an Emerging Drug Target for the Treatment of Cancer, Autoimmune Diseases, and Graft-Versus-Host Disease: Current Perspectives andFrontiers in immunology · 2018Article
- Article
Corrections and comments
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Authors and funding
16 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Overexpression of tumor necrosis factor α (TNFα) is a hallmark of many inflammatory diseases, including rheumatoid arthritis, inflammatory bowel disease, and septic shock and hepatitis, making it a potential therapeutic target for clinical interventions. To explore chemical inhibitors against TNFα activity, we applied computer-aided drug design combined with in vitro and cell-based assays and identified a lead chemical compound, (E)-4-(2-(4-chloro-3-nitrophenyl) (named as C87 thereafter), which directly binds to TNFα, potently inhibits TNFα-induced cytotoxicity (IC50 = 8.73 μM) and effectively blocks TNFα-triggered signaling activities. Furthermore, by using a murine acute hepatitis model, we showed that C87 attenuates TNFα-induced inflammation, thereby markedly reducing injuries to the liver and improving animal survival. Thus, our results lead to a novel and highly specific small-molecule TNFα inhibitor, which can be potentially used to treat TNFα-mediated inflammatory diseases.
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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.