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Linker-Dependent Folding Rationalizes PROTAC Cell Permeability

[Image: see text] Proteolysis-targeting chimeras (PROTACs) must be cell permeable to reach their target proteins. This is challenging as the bivalent structure of PROTACs puts them in chemical space at, or beyond, the outer limits of oral druggable space. We used NMR spectroscopy and molecular dynam...

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Detalles Bibliográficos
Autores principales: Poongavanam, Vasanthanathan, Atilaw, Yoseph, Siegel, Stephan, Giese, Anja, Lehmann, Lutz, Meibom, Daniel, Erdelyi, Mate, Kihlberg, Jan
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2022
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9574858/
https://www.ncbi.nlm.nih.gov/pubmed/36170570
http://dx.doi.org/10.1021/acs.jmedchem.2c00877