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First-in-class metallo-PROTAC as an effective degrader of select Pt-binding proteins
Paul D O'Dowd1,2, Graeme P Sullivan3, Daniel A Rodrigues1
1Department of Chemistry, Royal College of Surgeons in Ireland, Dublin 2, Ireland. dgriffith@rcsi.ie.
Abstract:
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.
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