Trivalent PROTACs enhance protein degradation via combined avidity and cooperativity

Bivalent PROTACs work drive protein degradation by simultaneously binding a target protein and an E3 ligase and forming a productive ternary complex. We hypothesized that increasing binding valency within a PROTAC could enhanced degradation. Here, we designed trivalent PROTACs consisting of a bivale...

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Bibliografiske detaljer
Udgivet i:Nat Chem Biol
Main Authors: Imaide, Satomi, Riching, Kristin M., Makukhin, Nikolai, Vetma, Vesna, Whitworth, Claire, Hughes, Scott J., Trainor, Nicole, Mahan, Sarah D., Murphy, Nancy, Cowan, Angus D., Chan, Kwok-Ho, Craigon, Conner, Testa, Andrea, Maniaci, Chiara, Urh, Marjeta, Daniels, Danette L., Ciulli, Alessio
Format: Artigo
Sprog:Inglês
Udgivet: 2021
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Article
Online adgang:https://ncbi.nlm.nih.gov/pmc/articles/PMC7611906/
https://ncbi.nlm.nih.gov/pubmed/34675414
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1038/s41589-021-00878-4
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