ArticleJournal of the American Chemical Society2024
Discovery of Thioether-Cyclized Macrocyclic Covalent Inhibitors by mRNA Display.
Article in Journal of the American Chemical Society, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
What it found
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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
11 citing papers in PubMed.
- De Novo Discovery of Nonstandard Thioisoindole-Bridged Bicyclic Peptides Targeting Traf2- and NCK-Interacting Kinase.Angewandte Chemie (International ed. in English) · 2026Article
- Enhanced screening via a pure DNA-encoded peptide library enabled by an Fmoc modification.Proceedings of the National Academy of Sciences of the United States of America · 2026Article
- The Current Toolbox for Covalent Inhibitors: From Hit Identification to Drug Discovery.JACS Au · 2025Review
- High-Throughput Activity Reprogramming of Proteases (HARP).ACS chemical biology · 2025Article
- mRNA display-enabled discovery of proximity-triggered covalent peptide-drug conjugates.Acta pharmaceutica Sinica. B · 2025Article
- Discovery of Macrocyclic Peptide Binders, Covalent Modifiers, and Degraders of a Structured RNA by mRNA Display.Journal of the American Chemical Society · 2025Article
- Unsaturated Phosphine Oxides for Modular Antibody Rebridging and Single Reagent Peptide-Cyclization-Bioconjugation.Angewandte Chemie (International ed. in English) · 2025Article
- From Concepts to Inhibitors: A Blueprint for Targeting Protein-Protein Interactions.Chemical reviews · 2025Review
- An mRNA Display Approach for Covalent Targeting of aJournal of the American Chemical Society · 2025Article
- Selection of Nucleotide-Encoded Mass Libraries of Macrocyclic Peptides for Inaccessible Drug Targets.Chemical reviews · 2024Review
- An mRNA Display Approach for Covalent Targeting of abioRxiv : the preprint server for biology · 2024Article
Corrections and comments
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Authors and funding
13 authors.
Funding
Abstract
Macrocyclic peptides are promising scaffolds for the covalent ligand discovery. However, platforms enabling the direct identification of covalent macrocyclic ligands in a high-throughput manner are limited. In this study, we present an mRNA display platform allowing selection of covalent macrocyclic inhibitors using 1,3-dibromoacetone-vinyl sulfone (DBA-VS). Testcase selections on TEV protease resulted in potent covalent inhibitors with diverse cyclic structures, among which cTEV6-2, a macrocyclic peptide with a unique C-terminal cyclization, emerged as the most potent covalent inhibitor of TEV protease described to-date. This study outlines the workflow for integrating chemical functionalization─installation of a covalent warhead─with mRNA display and showcases its application in targeted covalent ligand discovery.
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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.