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SPR-Measured Dissociation Kinetics of PROTAC Ternary Complexes Influence Target Degradation Rate

[Image: see text] Bifunctional degrader molecules, known as proteolysis-targeting chimeras (PROTACs), function by recruiting a target to an E3 ligase, forming a target/PROTAC/ligase ternary complex. Despite the importance of this key intermediate species, no detailed validation of a method to direct...

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Detalles Bibliográficos
Autores principales: Roy, Michael J., Winkler, Sandra, Hughes, Scott J., Whitworth, Claire, Galant, Michael, Farnaby, William, Rumpel, Klaus, Ciulli, Alessio
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2019
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6423499/
https://www.ncbi.nlm.nih.gov/pubmed/30721025
http://dx.doi.org/10.1021/acschembio.9b00092