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February 5, 2026Exploration of Drug ScienceOpen Access

Vinyl sulfones: selective and tunable covalent warheads against challenging enzyme targets

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Authors

RVRonald E. ViolaUniversity of Toledo

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Implication

Research demonstrates selective covalent inactivation of enzyme targets using vinyl sulfones, suggesting a new approach to drug development.

Key Points

  • The aim is to design vinyl sulfones as selective covalent warheads for challenging enzyme targets.
  • Development of vinyl sulfones as reactive warheads.
  • Designing selective inactivators for cysteine proteases and phosphoryl-utilizing enzymes.
  • Incorporation of vinyl sulfones into peptide structures that resemble natural substrates.
  • Vinyl sulfones are shown to selectively inactivate microbial and human cysteine proteases.
  • Effective targeting of a range of phosphoryl-utilizing enzymes was achieved.
  • Demonstrated success in targeting fungal aspartate semialdehyde dehydrogenase as a case study.

Cite This Study

Ronald E. Viola (2026) studied this question.

synapsesocial.com/papers/698433a5f1d9ada3c1fb0ee4https://doi.org/10.37349/eds.2026.1008147
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