ArticleProceedings of the National Academy of Sciences of the United States of America2005
Disabling TNF receptor signaling by induced conformational perturbation of tryptophan-107.
Article in Proceedings of the National Academy of Sciences of the United States of America, 2005. 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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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, 46 citations in OpenAlex.
- Intra-cluster receptor density (IRD): A molecular switch for TNFR1 clusters' signaling.Science advances · 2026Article
- Discovery of Ligands for the TNFR1 Extracellular Domain Using Fragment-Based Drug Discovery.ChemMedChem · 2026Article
- TNF as a mediator of metabolic inflammation and body-brain interaction in obesity-driven neuroinflammation and neurodegeneration.Ageing research reviews · 2025Review
- CTRP9 engages AdipoR1 and promotes T cell glycolysis and immunity.EMBO reports · 2025Article
- Targeting the inter-monomeric space of TNFR1 pre-ligand dimers: A novel binding pocket for allosteric modulators.Computational and structural biotechnology journal · 2025Article
- Review
- Peptide-based allosteric inhibitor targets TNFR1 conformationally active region and disables receptor-ligand signaling complex.Proceedings of the National Academy of Sciences of the United States of America · 2024Article
- TNF and TNF receptors as therapeutic targets for rheumatic diseases and beyond.Nature reviews. Rheumatology · 2023Review
- Zafirlukast Is a Promising Scaffold for Selectively Inhibiting TNFR1 Signaling.ACS bio & med chem Au · 2023Article
- Therapeutic potential of TNFα inhibitors in chronic inflammatory disorders: Past and future.Genes & diseases · 2021Review
- FOXP3 and Tip60 Structural Interactions Relevant to IPEX Development Lead to Potential Therapeutics to Increase FOXP3 Dependent Suppressor T Cell Functions.Frontiers in pediatrics · 2021Review
- Disabling the Nuclear Translocalization of RelA/NF-κB by a Small Molecule Inhibits Triple-Negative Breast Cancer Growth.Breast cancer (Dove Medical Press) · 2021Article
- Regulatory T Cells: Regulation of Identity and Function.Frontiers in immunology · 2021Review
- Small molecules that inhibit TNF signalling by stabilising an asymmetric form of the trimer.Nature communications · 2019Article
- Noncompetitive inhibitors of TNFR1 probe conformational activation states.Science signaling · 2019Article
- Novel TNF receptor-1 inhibitors identified as potential therapeutic candidates for traumatic brain injury.Journal of neuroinflammation · 2018Article
- Ainsliadimer A selectively inhibits IKKα/β by covalently binding a conserved cysteine.Nature communications · 2015Article
- Structural basis for treating tumor necrosis factor α (TNFα)-associated diseases with the therapeutic antibody infliximab.The Journal of biological chemistry · 2013Article
- Disabling the mitotic spindle and tumor growth by targeting a cavity-induced allosteric site of survivin.Oncogene · 2012Article
- TCR Nanoclusters as the Framework for Transmission of Conformational Changes and Cooperativity.Frontiers in immunology · 2012Article
Corrections and comments
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Authors and funding
9 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
We have disabled TNF receptor (TNFR) function by inducing allosteric modulation of tryptophan-107 (W107) in the receptor. The allosteric effect operates by means of an allosteric cavity found a short distance from a previously identified loop involved in ligand binding. Occupying this cavity by small molecules leads to perturbation of distal W107 and disables functions of the TNFR, a molecule not known to undergo conformational change upon binding TNF-alpha. TNF-alpha-induced NF-kappaB and p38 kinase activities and clinical symptoms of collagen-induced arthritis in mice were all diminished. Thus, disabling receptor function by induced conformational changes of active binding surfaces represents an innovative paradigm in structure-based drug design.
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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.