ArticleAdvanced science (Weinheim, Baden-Wurttemberg, Germany)2022
A Small Molecule Selected from a DNA-Encoded Library of Natural Products That Binds to TNF-α and Attenuates Inflammation In Vivo.
Article in Advanced science (Weinheim, Baden-Wurttemberg, Germany), 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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Who cites it
21 citing papers in PubMed, 35 citations in OpenAlex.
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- Discovery of a first-in-class SLIT2 binder disrupting the SLIT2/ROBO1 axisRSC medicinal chemistry · 2025Article
- Effects of Polyphenols from Oat and Oat Bran on Anti-Inflammatory Activity and Intestinal Barrier Function in Raw264.7 and Caco-2 Models.Nutrients · 2025Article
- Abnormal proportions and functions of myeloid-derived suppressor cells in peripheral blood of patients with diffuse large B-cell lymphoma.BMC cancer · 2025Article
- Identification of potential MMP-8 inhibitors through virtual screening of natural product databases.In silico pharmacology · 2025Article
- Targeting TNF/TNFR superfamilies in immune-mediated inflammatory diseases.The Journal of experimental medicine · 2024Review
- FSOACS medicinal chemistry letters · 2024Article
- Encoding and display technologies for combinatorial libraries in drug discovery: The coming of age from biology to therapy.Acta pharmaceutica Sinica. B · 2024Review
- Potential mechanism of ginseng in the treatment of periodontitis based on network pharmacology and molecular docking.Hua xi kou qiang yi xue za zhi = Huaxi kouqiang yixue zazhi = West China journal of stomatology · 2024Article
- Mask and Release Strategy-Enabled Diversity-Oriented Synthesis for DNA-Encoded Library.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2024Article
- Evolution of chemistry and selection technology for DNA-encoded library.Acta pharmaceutica Sinica. B · 2024Review
- Research advances ofFrontiers in immunology · 2024Review
- Current Immunotherapy Strategies for Rheumatoid Arthritis: The Immunoengineering and Delivery Systems.Research (Washington, D.C.) · 2023Review
- Recent Advances in ROS-Scavenging Metallic Nanozymes for Anti-Inflammatory Diseases: A Review.Chonnam medical journal · 2023Review
- Metal-Free and Open-Air Arylation Reactions of Diaryliodonium Salts for DNA-Encoded Library Synthesis.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2022Article
- 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
- Discovery of TIGIT inhibitors based on DEL and machine learning.Frontiers in chemistry · 2022Article
Corrections and comments
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Authors and funding
13 authors at 5 institutions in 1 country.
Funding
Abstract
Tumor necrosis factor α (TNF-α) inhibitors have shown great success in the treatment of autoimmune diseases. However, to date, approved drugs targeting TNF-α are restricted to biological macromolecules, largely due to the difficulties in using small molecules for pharmaceutical intervention of protein-protein interactions. Herein the power of a natural product-enriched DNA-encoded library (nDEL) is exploited to identify small molecules that interfere with the protein-protein interaction between TNF-α and the cognate receptor. Initially, to select molecules capable of binding to TNF-α , "late-stage" DNA modification method is applied to construct an nDEL library consisted of 400 sterically diverse natural products and pharmaceutically active chemicals. Several natural products, including kaempferol, identified not only show direct interaction with TNF-α, but also lead to the blockage of TNF-α/TNFR1 interaction. Significantly, kaempferol attenuates the TNF-α signaling in cells and reduces the 12-O-tetradecanoylphorbol-13-acetateinduced ear inflammation in mice. Structure-activity-relationship analyses demonstrate the importance of substitution groups at C-3, C-7, and C-4' of kaempferol. The nDEL hit, kaempferol, represents a novel chemical scaffold capable of specifically recognizing TNF-α and blocking its signal transduction, a promising starting point for the development of a small molecule TNF-α inhibitor for use in the clinical setting.
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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.