Direct-to-Biology Accelerates PROTAC Synthesis and the Evaluation of Linker Effects on Permeability and Degradation

[Image: see text] A platform to accelerate optimization of proteolysis targeting chimeras (PROTACs) has been developed using a direct-to-biology (D2B) approach with a focus on linker effects. A large number of linker analogs—with varying length, polarity, and rigidity—were rapidly prepared and chara...

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Detalles Bibliográficos
Autores principales: Hendrick, Charles E., Jorgensen, Jeff R., Chaudhry, Charu, Strambeanu, Iulia I., Brazeau, Jean-Francois, Schiffer, Jamie, Shi, Zhicai, Venable, Jennifer D., Wolkenberg, Scott E.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2022
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9290060/
https://www.ncbi.nlm.nih.gov/pubmed/35859867
http://dx.doi.org/10.1021/acsmedchemlett.2c00124

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