ArticleRSC chemical biology2026
High-throughput discovery and characterisation of pentafluorobenzene sulfonamide modifiers of Aurora A kinase.
Article in RSC chemical biology, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
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Who cites it
2 citing papers in PubMed.
- Accelerate Your Science: Direct-to-Biology Strategies in Medicinal Chemistry.Journal of medicinal chemistry · 2026Review
- Modular Rh-Catalyzed Synthesis and Biological Profiling of Diverse Pentafluorobenzenesulfonamide Reactive Fragments.Chemistry (Weinheim an der Bergstrasse, Germany) · 2026Article
Corrections and comments
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Authors and funding
11 authors.
Funding
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Abstract
Covalent modification can enable understanding and modulation of protein function, and the identification of new therapeutic opportunities. A "direct to biology" workflow was developed that harnesses sulfonylation as a connective reaction for the synthesis of diverse sets of reactive fragments. The workflow expanded the diversity of accessible reactive fragment sets, and facilitated the discovery of pentafluorobenzene sulfonamides that modify Aurora A kinase, NEK7 kinase, and UbcH5B. Characterisation of several of the Aurora A-modifying reactive fragments revealed both their modification rates and sites. Furthermore, Cys247, a residue typically buried in Aurora A crystal structures, was identifed as a modifable residue. These findings underscore the importance of protein dynamics in determining cysteine reactivity and highlight the utility of reactive fragment sets for identifying cryptic pockets. Sulfonylation is therefore a useful complement to amide formation in "direct to biology" workflows aimed at identifying novel opportunities for targeted protein modification.
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Registered trials
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