ArticleRSC chemical biology2021
Development and biological applications of sulfur-triazole exchange (SuTEx) chemistry.
Article in RSC chemical biology, 2021. 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.
- Progress and challenges in traceless ligand-directed labelling chemistry.Communications chemistry · 2026Review
- SuFEx chemistry for nucleosides, nucleotides, and nucleic acids.RSC chemical biology · 2026Review
- Recent Advances in Bioconjugation of Aromatic Amino Acid Residues by a Reactivity-Guided Approach.Chemical record (New York, N.Y.) · 2026Review
- Click chemistry for natural product-inspired covalent drug discovery.Drug discovery today · 2025Review
- Advancing Covalent Ligand and Drug Discovery beyond Cysteine.Chemical reviews · 2025Review
- Emerging opportunities for intact and native protein analysis using chemical proteomics.Analytica chimica acta · 2025Review
- Harnessing Oxetane and Azetidine Sulfonyl Fluorides for Opportunities in Drug Discovery.Journal of the American Chemical Society · 2024Article
- Discovery of Trypanosoma brucei inhibitors enabled by a unified synthesis of diverse sulfonyl fluorides.Communications chemistry · 2024Article
- Covalent Stapling of the Cereblon Sensor Loop Histidine Using Sulfur-Heterocycle Exchange.ACS medicinal chemistry letters · 2023Article
- Predicting small molecule binding pockets on diacylglycerol kinases using chemoproteomics and AlphaFold.RSC chemical biology · 2023Article
- Sulfonylation of RNA 2'-OH groups.ACS central science · 2023Article
- Proteome-Wide Fragment-Based Ligand and Target Discovery.Israel journal of chemistry · 2023Article
- Global profiling identifies a stress-responsive tyrosine site on EDC3 regulating biomolecular condensate formation.Cell chemical biology · 2022Article
- Sulfur-Phenolate Exchange As a Fluorine-Free Approach to S(VI) Exchange Chemistry on Sulfonyl Moieties.Organic letters · 2022Article
- Covalent drugs targeting histidine - an unexploited opportunity?RSC medicinal chemistry · 2022Article
- Cereblon covalent modulation through structure-based design of histidine targeting chemical probes.RSC chemical biology · 2022Article
- Inverse Drug Discovery identifies weak electrophiles affording protein conjugates.Current opinion in chemical biology · 2022Review
- Reactive chemistry for covalent probe and therapeutic development.Trends in pharmacological sciences · 2022Review
- Advances in chemical proteomic evaluation of lipid kinases-DAG kinases as a case study.Current opinion in chemical biology · 2021Review
- Direct Target Site Identification of a Sulfonyl-Triazole Covalent Kinase Probe by LC-MS Chemical Proteomics.Analytical chemistry · 2021Article
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Authors and funding
4 authors.
Funding
Abstract
Sulfur electrophiles constitute an important class of covalent small molecules that have found widespread applications in synthetic chemistry and chemical biology. Various electrophilic scaffolds, including sulfonyl fluorides and arylfluorosulfates as recent examples, have been applied for protein bioconjugation to probe ligand sites amenable for chemical proteomics and drug discovery. In this review, we describe the development of sulfonyl-triazoles as a new class of electrophiles for sulfur-triazole exchange (SuTEx) chemistry. SuTEx achieves covalent reaction with protein sites through irreversible modification of a residue with an adduct group (AG) upon departure of a leaving group (LG). A principal differentiator of SuTEx from other chemotypes is the selection of a triazole heterocycle as the LG, which introduces additional capabilities for tuning the sulfur electrophile. We describe the opportunities afforded by modifications to the LG and AG alone or in tandem to facilitate nucleophilic substitution reactions at the SO
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Registered trials
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