ArticleProceedings of the National Academy of Sciences of the United States of America2019
SuFEx-enabled, agnostic discovery of covalent inhibitors of human neutrophil elastase.
Article in Proceedings of the National Academy of Sciences of the United States of America, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 92 papers.
What it found
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Who cites it
92 citing papers in PubMed.
- Cyclopropanol can function as a caged dual-functional warhead for selective electrochemical bioconjugation.Nature chemistry · 2026Article
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- Counteranion-mediated dynamic kinetic asymmetric fluorination to access sulfur-stereogenic center.Nature communications · 2026Article
- Structure-Aided Design of a LuxR-Type Quorum Sensing SuFEx-Based Potential Inhibitor: Covalent or Competitive Inhibition?Biomolecules · 2026Article
- Substituent Effects on Sulfur Phenolate Exchange Reactions: Reactivity and Bonding Analysis.Chemistry (Weinheim an der Bergstrasse, Germany) · 2025Article
- β-alkoxy enones for biocompatible primary amine conjugation.Innovation (Cambridge (Mass.)) · 2025Article
- Click chemistry for natural product-inspired covalent drug discovery.Drug discovery today · 2025Review
- Discovery of Macrocyclic Peptide Binders, Covalent Modifiers, and Degraders of a Structured RNA by mRNA Display.Journal of the American Chemical Society · 2025Article
- Disubstituted Meldrum's Acid: Another Scaffold with SuFEx-like Reactivity.Molecules (Basel, Switzerland) · 2025Article
- Structure-based rational design of covalent probes.Communications chemistry · 2025Review
- Advances in sulfonyl exchange chemical biology: expanding druggable target space.Chemical science · 2025Review
- Mimicry of molecular glues using dual covalent chimeras.Nature communications · 2025Article
- Total syntheses of cyclohelminthol I-IV reveal a new cysteine-selective covalent reactive group.Chemical science · 2025Article
- Click Chemistry Methodology: The Novel Paintbrush of Drug Design.ACS chemical biology · 2025Review
- Diversity Oriented Clicking for Modular Synthesis.Nature reviews. Methods primers · 2025Article
- Arginine Accelerates Sulfur Fluoride Exchange and Phosphorus Fluoride Exchange Reactions between Proteins.Angewandte Chemie (International ed. in English) · 2024Article
- SONature communications · 2024Article
- Strain-release alkylation of Asp12 enables mutant selective targeting of K-Ras-G12D.Nature chemical biology · 2024Article
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- Identification of clickable HIV-1 capsid-targeting probes for viral replication inhibition.Cell chemical biology · 2024Article
32 more citing papers are in PubMed but not listed here.
Corrections and comments
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Authors and funding
10 authors.
Funding
Abstract
Sulfur fluoride exchange (SuFEx) has emerged as the new generation of click chemistry. We report here a SuFEx-enabled, agnostic approach for the discovery and optimization of covalent inhibitors of human neutrophil elastase (hNE). Evaluation of our ever-growing collection of SuFExable compounds toward various biological assays unexpectedly revealed a selective and covalent hNE inhibitor: benzene-1,2-disulfonyl fluoride. Synthetic derivatization of the initial hit led to a more potent agent, 2-(fluorosulfonyl)phenyl fluorosulfate with IC
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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.