ArticleAngewandte Chemie (International ed. in English)2020
Isotopically Labeled Desthiobiotin Azide (isoDTB) Tags Enable Global Profiling of the Bacterial Cysteinome.
Article in Angewandte Chemie (International ed. in English), 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 65 papers.
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65 citing papers in PubMed, 118 citations in OpenAlex.
- Bromo-desthiobiotin (Br-DTB) tag for unbiased profiling and identification of chemical modifications.RSC chemical biology · 2026Article
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- Progress and application of activity-based protein profiling for the discovery of natural product targets.Molecular diversity · 2026Review
- Metronidazole and ether derivatives target Helicobacter pylori via simultaneous stress induction and inhibition.Nature microbiology · 2026Article
- Total Synthesis and Biological Evaluation of Leptosphaerone B and Derivatives of Microketide A.Journal of natural products · 2026Article
- Modular Vinyl Phosphonamidates for Cysteine-Directed Protein Targeting.Journal of the American Chemical Society · 2026Article
- Article
- Targeting the Reactive Proteome: Recent Advances in Activity-Based Protein Profiling and Probe Design.Biomolecules · 2025Review
- Profiling the proteome-wide selectivity of diverse electrophiles.Nature chemistry · 2025Article
- Covalent Degraders of Immune Regulatory Transcription Factors IRF8 and IRF5.bioRxiv : the preprint server for biology · 2025Article
- CIAA: Integrated Proteomics and Structural Modeling for Understanding Cysteine Reactivity with Iodoacetamide Alkyne.ACS chemical biology · 2025Article
- Inhibition of RACK1-Mediated NLRP3 Oligomerization (Active Conformation) Ameliorates Acute Respiratory Distress Syndrome.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2025Article
- Proteome-wide ligandability maps of drugs with diverse cysteine-reactive chemotypes.Nature communications · 2025Article
- Antibiotic target discovery by integrated phenotypic and activity-based profiling of electrophilic fragments.Cell chemical biology · 2025Article
- Covalent Proximity Inducers.Chemical reviews · 2025Review
- Activity-Based Protein Profiling for Functional Cysteines and Protein Target Identification.Methods in molecular biology (Clifton, N.J.) · 2025Article
- Targeted Protein Localization by Covalent 14-3-3 Recruitment.Journal of the American Chemical Society · 2024Article
- Article
5 more citing papers are in PubMed but not listed here.
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3 authors at 1 institution in 1 country.
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No grant is acknowledged in the PubMed record.
Abstract
Rapid development of bacterial resistance has led to an urgent need to find new druggable targets for antibiotics. In this context, residue-specific chemoproteomic approaches enable proteome-wide identification of binding sites for covalent inhibitors. Described here are easily synthesized isotopically labeled desthiobiotin azide (isoDTB) tags that shortened the chemoproteomic workflow and allowed an increased coverage of cysteines in bacterial systems. They were used to quantify 59 % of all cysteines in essential proteins in Staphylococcus aureus and enabled the discovery of 88 cysteines that showed high reactivity, which correlates with functional importance. Furthermore, 268 cysteines that are engaged by covalent ligands were identified. Inhibition of HMG-CoA synthase was verified and will allow addressing the bacterial mevalonate pathway through a new target. Overall, a broad map of the bacterial cysteinome was obtained, which will facilitate the development of antibiotics with novel modes-of-action.
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