ArticleNature communications2021
A conformation-selective monoclonal antibody against a small molecule-stabilised signalling-deficient form of TNF.
Article in Nature communications, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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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
16 citing papers in PubMed, 31 citations in OpenAlex.
- First-in-Human Single and Multiple Ascending Dose Studies of Balinatunfib, a Small Molecule Inhibitor of TNFR1 Signaling in Healthy Participants.Clinical pharmacology and therapeutics · 2025Trial
- SGLT2 Inhibition as a Perioperative Cardiorenal Stabilizer in Cardiac Surgery: Integrated Clinical Cohort and Pleiotropic Network-Based Pharmacological Analysis.Journal of clinical medicine · 2026Article
- Integrative Multiomics and Single-Cell Profiling Identify TNFRSF1AComputational and structural biotechnology journal · 2026Article
- Icariin-mediated structural stabilization of TNF-α triggers a pro-regenerative signaling switch for endothelial recovery after myocardial infarction.Frontiers in pharmacology · 2026Article
- Design of minibinder proteins as universal antagonists against canine and human TNFα.Communications biology · 2025Article
- Highly ordered clustering of TNFα and BAFF ligand-receptor-intracellular adaptor complexes on a lipid membrane.Nature communications · 2025Article
- Food-derived linear vs. rationally designed cyclic peptides as potent TNF-alpha inhibitors: an integrative computational study.Frontiers in bioinformatics · 2025Article
- Discovery of Cyclic Peptide Inhibitors Targeted on TNFα-TNFR1 from Computational Design and Bioactivity Verification.Molecules (Basel, Switzerland) · 2024Article
- Characterization of 3,3'-iminodipropionitrile (IDPN) damaged utricle transcriptome in the adult mouse utricle.Frontiers in molecular neuroscience · 2024Article
- It's ok to be outnumbered - sub-stoichiometric modulation of homomeric protein complexes.RSC medicinal chemistry · 2023Review
- Phytochemical Analysis of the Methanolic Extract and Essential Oil from Leaves of Industrial HempPlants (Basel, Switzerland) · 2022Article
- Network pharmacology and experimental verification based research into the effect and mechanism of Aucklandiae Radix-Amomi Fructus against gastric cancer.Scientific reports · 2022Article
- Conformation-locking antibodies for the discovery and characterization of KRAS inhibitors.Nature biotechnology · 2022Article
- Membrane Hormone Receptors and Their Signaling Pathways as Targets for Endocrine Disruptors.Journal of xenobiotics · 2022Review
- An orally available small molecule that targets soluble TNF to deliver anti-TNF biologic-like efficacy in rheumatoid arthritis.Frontiers in pharmacology · 2022Article
- Modulating Target Protein Biology Through the Re-mapping of Conformational Distributions Using Small Molecules.Frontiers in chemistry · 2021Article
Corrections and comments
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Authors and funding
15 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
We have recently described the development of a series of small-molecule inhibitors of human tumour necrosis factor (TNF) that stabilise an open, asymmetric, signalling-deficient form of the soluble TNF trimer. Here, we describe the generation, characterisation, and utility of a monoclonal antibody that selectively binds with high affinity to the asymmetric TNF trimer-small molecule complex. The antibody helps to define the molecular dynamics of the apo TNF trimer, reveals the mode of action and specificity of the small molecule inhibitors, acts as a chaperone in solving the human TNF-TNFR1 complex crystal structure, and facilitates the measurement of small molecule target occupancy in complex biological samples. We believe this work defines a role for monoclonal antibodies as tools to facilitate the discovery and development of small-molecule inhibitors of protein-protein interactions.
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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.