ArticleChembiochem : a European journal of chemical biology2021
Discovery of a Cell-Active SuTEx Ligand of Prostaglandin Reductase 2.
Article in Chembiochem : a European journal of chemical biology, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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Who cites it
10 citing papers in PubMed, 22 citations in OpenAlex.
- Progress and challenges in traceless ligand-directed labelling chemistry.Communications chemistry · 2026Review
- Advancing Covalent Ligand and Drug Discovery beyond Cysteine.Chemical reviews · 2025Review
- Human PTGR2 Inactivation Alters Eicosanoid Metabolism and Cytokine Response of Inflammatory Macrophages.ACS chemical biology · 2025Article
- Advances in sulfonyl exchange chemical biology: expanding druggable target space.Chemical science · 2025Review
- Discovery and Optimization of a Covalent AKR1C3 Inhibitor.Journal of medicinal chemistry · 2025Article
- Emerging opportunities for intact and native protein analysis using chemical proteomics.Analytica chimica acta · 2025Review
- Imidazoles are Tunable Nucleofuges for Developing Tyrosine-Reactive Electrophiles.Chembiochem : a European journal of chemical biology · 2024Article
- Global Discovery of Covalent Modulators of Ribonucleoprotein Granules.Journal of the American Chemical Society · 2023Article
- 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
Corrections and comments
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Authors and funding
6 authors at 1 institution in 1 country.
Funding
Abstract
Sulfonyl-triazoles have emerged as a new reactive group for covalent modification of tyrosine sites on proteins through sulfur-triazole exchange (SuTEx) chemistry. The extent to which this sulfur electrophile can be tuned for developing ligands with cellular activity remains largely underexplored. Here, we performed fragment-based ligand discovery in live cells to identify SuTEx compounds capable of liganding tyrosine sites on diverse protein targets. We verified our quantitative chemical proteomic findings by demonstrating concentration-dependent activity of SuTEx ligands, but not inactive counterparts, against recombinant protein targets directly in live cells. Our structure-activity relationship studies identified the SuTEx ligand HHS-0701 as a cell-active inhibitor capable of blocking prostaglandin reductase 2 (PTGR2) biochemical activity.
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Registered trials
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