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Scaffold hopping enables direct access to more potent PROTACs with in vivo activity

Herein we employ a scaffold hopping approach to enhance the activity of a previously reported BCR-Abl PROTAC. This represents a significant advance in the PROTAC field since it can abrogate the need to optimize the linker to access a more potent degrader. The new PROTAC demonstrates a >10 fold in...

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Bibliografiske detaljer
Udgivet i:Chem Commun (Camb)
Main Authors: Burslem, George M., Bondeson, Daniel P., Crews, Craig M.
Format: Artigo
Sprog:Inglês
Udgivet: 2020
Fag:
Online adgang:https://ncbi.nlm.nih.gov/pmc/articles/PMC7404552/
https://ncbi.nlm.nih.gov/pubmed/32519703
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1039/d0cc02201b
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