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

Paul D. O’Dowd; Graeme P. Sullivan; Daniel A. Rodrigues; Tríona Ní Chonghaile; Darren M. Griffith

doi:10.1039/D3CC03340F

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

Paul D. O’Dowd, Graeme P. Sullivan, Daniel A. Rodrigues, Tríona Ní Chonghaile and Darren M. Griffith
Chem. Commun., 2023,59, 12641-12644
DOI: 10.1039/D3CC03340F, Communication

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Abstract | Cited by

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.

Graphical abstract: First-in-class metallo-PROTAC as an effective degrader of select Pt-binding proteins

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