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First-in-class metallo-PROTAC as an effective degrader of select Pt-binding proteins.

Paul D O'DowdGraeme P SullivanDaniel A RodriguesTríona Ní ChonghaileDarren M Griffith
Published in: Chemical communications (Cambridge, England) (2023)
We report the development of the first metallo-PROTAC, specifically a Pt-PROTAC, that can effectively degrade select Pt(II)-binding proteins. The Pt-PROTAC prototype successfully degraded thioredoxin-1 and thioredoxin reductase-1 in multiple myeloma cancer cell lines. Metallo-PROTACs will have important applications in the identification of metal binding proteins and as chemotherapeutic agents.
Keyphrases
  • multiple myeloma
  • gram negative
  • papillary thyroid
  • squamous cell
  • childhood cancer