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First-in-class metallo-PROTAC as an effective degrader of select Pt-binding proteins.
journal contributionposted on 2023-10-13, 15:17 authored by Paul O'DowdPaul O'Dowd, Graeme SullivanGraeme Sullivan, Daniel Alencar RodriguesDaniel Alencar Rodrigues, Triona Ni ChonghaileTriona Ni Chonghaile, Darren GriffithDarren Griffith
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.
SSPC PharM5 | Funder: Science Foundation Ireland | Grant ID: 12/RC/2275_P2
Irish Research Council (IRCLA/ 2022/2822)
Irish Research Council (GOIPD/2022/764)
Irish Cancer Society under grant number CRF21SUL
European Regional Development Fund under Grant Number 12/RC/2275_P2
CommentsThe original article is available at https://pubs.rsc.org/ Pre-print is available on ChemRxiv. https://doi.org/10.26434/chemrxiv-2023-r5l4k and RCSI Repository https://hdl.handle.net/10779/rcsi.24204363.v1
Published CitationO'Dowd PD, Sullivan GP, Rodrigues DA, Chonghaile TN, Griffith DM. First-in-class metallo-PROTAC as an effective degrader of select Pt-binding proteins. Chem Commun (Camb). 2023.
Publication Date28 September 2023
- Physiology and Medical Physics
- School of Pharmacy and Biomolecular Sciences
- Chemistry and Pharmaceutical Sciences
PublisherRoyal Society of Chemistry (RSC)
- Published Version (Version of Record)