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March 4, 2026Open Access

Modular Vinyl Phosphonamidates for Cysteine-Directed Protein Targeting

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Authors

CSChristian E. StiegerCVCharlotte VölkelMBMathias B. Bertelsen

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Overview

Introduces vinyl phosphonamidates as selective cysteine-targeting tools, suggesting improvement for drug development.

Key Points

  • The aim is to evaluate vinyl phosphonamidates (VPAs) as a new class of cysteine-directed electrophiles for drug discovery.
  • Assessed VPA reactivity and selectivity compared to established electrophiles.
  • Developed VPA-functionalized derivatives of existing FDA-approved inhibitors.
  • Utilized gel-based and mass spectrometry-based activity-based protein profiling for evaluation.
  • Created a bifunctional PROTAC for targeted protein degradation.
  • VPAs showed significantly lower reactivity towards glutathione than traditional electrophiles.
  • VPA-derived compounds exhibited limited nonspecific reactivity in human cell lysate.
  • VPA-functionalized drug ligands maintained inhibitor efficiency with fewer off-target effects.
  • Demonstrated modular nature of VPAs allowed for customization in targeted drug development.

Cite This Study

Stieger et al. (2026) studied this question.

synapsesocial.com/papers/69a7cd5ed48f933b5eed998bhttps://doi.org/10.17169/refubium-51403
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