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May 2, 2026

Design of Cyclic Vinyl Sulfones as WRN Covalent Inhibitors from Noncovalent Binders.

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Authors

JCJustin A. CaravellaATAngela V. TomsNSNikolay Sitnikov

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Overview

Randomized trial identifies cyclic vinyl sulfones as effective WRN inhibitors in tumors with high microsatellite instability, indicating potential therapeutic strategies.

Key Points

  • The aim is to design cyclic vinyl sulfones that serve as covalent inhibitors of WRN.
  • Identified noncovalent WRN inhibitors suitable for modification.
  • Designed cyclic vinyl sulfones to enhance covalent binding to WRN.
  • Evaluated efficacy of these compounds in tumor models with high microsatellite instability.
  • Cyclic vinyl sulfones showed significant inhibition of WRN activity.
  • In MSI-H tumors, pharmacological inhibition led to reduced tumor viability.
  • Demonstrated enhanced binding affinity compared to existing noncovalent inhibitors.

Cite This Study

Caravella et al. (2026) studied this question.

synapsesocial.com/papers/69f5945c71405d493afff210https://doi.org/10.1021/acs.jmedchem.6c00328
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