ArticleJournal of the American Chemical Society2021
Exploring the Versatility of the Covalent Thiol-Alkyne Reaction with Substituted Propargyl Warheads: A Deciding Role for the Cysteine Protease.
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 31 papers.
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Who cites it
31 citing papers in PubMed, 67 citations in OpenAlex.
- USP24 is a cross-reactive DUB targeting MOV10 to regulate IFN-I production.Nature communications · 2026Article
- From Covalent Traps to Fluorescent Beacons: The Expanding Arsenal of Chemical Probes for Studying Ubiquitin and Ubiquitin-Like Proteins.Angewandte Chemie (International ed. in English) · 2026Review
- Discovery of Coronavirus Main Protease Inhibitors with Enhanced Brain Exposure and Potent Oral Efficacy in SARS-CoV-2 and MERS Infection Models.Journal of medicinal chemistry · 2026Article
- Design, synthesis and evaluation of clickable photoaffinity probes for nuclear lamins.Bioorganic & medicinal chemistry letters · 2025Article
- Advancing Covalent Ligand and Drug Discovery beyond Cysteine.Chemical reviews · 2025Review
- Structure-based discovery of highly bioavailable, covalent, broad-spectrum coronavirus MScience advances · 2025Article
- Design, Construction, and Validation of a Yeast-Displayed Chemically Expanded Antibody Library.ACS synthetic biology · 2025Article
- Development of potential immunomodulatory ligands targeting natural killer T cells inspired by gut symbiont-derived glycolipids.Communications chemistry · 2025Article
- Morita-Baylis-Hillman Adduct Chemistry as a Tool for the Design of Lysine-Targeted Covalent Ligands.ACS medicinal chemistry letters · 2025Article
- Chemical- and photo-activation of protein-protein thiol-ene coupling for protein profiling.Communications chemistry · 2025Article
- Exploration of the tunability of BRD4 degradation by DCAF16 trans-labelling covalent glues.European journal of medicinal chemistry · 2024Article
- Template-assisted covalent modification underlies activity of covalent molecular glues.Nature chemical biology · 2024Article
- Structural and Biochemical Insights into the Mechanism of Action of the Clinical USP1 Inhibitor, KSQ-4279.Journal of medicinal chemistry · 2024Article
- Design, Construction, and Validation of a Yeast-Displayed Chemically Expanded Antibody Library.bioRxiv : the preprint server for biology · 2024Article
- Exploring diverse reactive warheads for the design of SARS-CoV-2 main protease inhibitors.European journal of medicinal chemistry · 2023Article
- Exploration of the Tunability of BRD4 Degradation by DCAF16bioRxiv : the preprint server for biology · 2023Article
- Cellular Validation of a Chemically Improved Inhibitor Identifies Monoubiquitination on OTUB2.ACS chemical biology · 2023Article
- Alkyne as a Latent Warhead to Covalently Target SARS-CoV-2 Main Protease.Journal of medicinal chemistry · 2023Article
- Technologies for Direct Detection of Covalent Protein-Drug Adducts.Pharmaceuticals (Basel, Switzerland) · 2023Review
- Total Chemical Synthesis of LC3A and LC3B Activity-Based Probes.Biomedicines · 2023Article
Corrections and comments
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Authors and funding
6 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Terminal unactivated alkynes are nowadays considered the golden standard for cysteine-reactive warheads in activity-based probes (ABPs) targeting cysteine deubiquitinating enzymes (DUBs). In this work, we study the versatility of the thiol-alkyne addition reaction in more depth. Contrary to previous findings with UCHL3, we now show that covalent adduct formation can progress with substituents on the terminal or internal alkyne position. Strikingly, acceptance of alkyne substituents is strictly DUB-specific as this is not conserved among members of the same subfamily. Covalent adduct formation with the catalytic cysteine residue was validated by gel analysis and mass spectrometry of intact ABP-treated USP16CD
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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.