ArticleJournal of the American Chemical Society2021
Tunable Methacrylamides for Covalent Ligand Directed Release Chemistry.
Article in Journal of the American Chemical Society, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 37 papers.
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Who cites it
37 citing papers in PubMed.
- Chemical reactions for the ligand-directed modification of native proteins.Chemical Society reviews · 2026Review
- Progress and challenges in traceless ligand-directed labelling chemistry.Communications chemistry · 2026Review
- On-resin Heck coupling enables small-molecule ligand discovery with covalent peptide-encoded libraries.Chemical science · 2026Article
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- Pharmacophore-targeted fluorescence sensing of ibrutinibRSC advances · 2026Article
- Recent advances in site-specific modifications of peptides and proteins.Chemical science · 2026Review
- α-Halothioamide warheads with enhanced cysteine reactivity and specificity for covalent protein labelling.Nature communications · 2026Article
- Machine Learning-Informed Nano Co-Assembly Inhibits Fibroblast Activation Protein and Improves Drug Delivery in Fibrotic Tissue.Advanced materials (Deerfield Beach, Fla.) · 2026Article
- Exploiting intracellular oncogenic proteins to release cytotoxins.RSC medicinal chemistry · 2026Article
- Modular Vinyl Phosphonamidates for Cysteine-Directed Protein Targeting.Journal of the American Chemical Society · 2026Article
- A Scalable Design for Proximity-Inducing Molecules.bioRxiv : the preprint server for biology · 2026Article
- Article
- Transition-Metal-Based Dearomatization Strategy for the Synthesis of FunctionalizedOrganometallics · 2025Article
- Advancing Covalent Ligand and Drug Discovery beyond Cysteine.Chemical reviews · 2025Review
- Allosteric Covalent Inhibitors of the STAT3 Transcription Factor from Virtual Screening.ACS medicinal chemistry letters · 2025Article
- Morita-Baylis-Hillman Adduct Chemistry as a Tool for the Design of Lysine-Targeted Covalent Ligands.ACS medicinal chemistry letters · 2025Article
- Covalent Proximity Inducers.Chemical reviews · 2025Review
- SuFEx Chemistry Enables Covalent Assembly of a 280-kDa 18-Subunit Pore-Forming Complex.Journal of the American Chemical Society · 2024Article
- Development of ketalized unsaturated saccharides as multifunctional cysteine-targeting covalent warheads.Communications chemistry · 2024Article
- Design,Current drug discovery technologies · 2024Article
Corrections and comments
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Authors and funding
12 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Targeted covalent inhibitors are an important class of drugs and chemical probes. However, relatively few electrophiles meet the criteria for successful covalent inhibitor design. Here we describe α-substituted methacrylamides as a new class of electrophiles suitable for targeted covalent inhibitors. While typically α-substitutions inactivate acrylamides, we show that hetero α-substituted methacrylamides have higher thiol reactivity and undergo a conjugated addition-elimination reaction ultimately releasing the substituent. Their reactivity toward thiols is tunable and correlates with the p
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Registered trials
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