Amide-to-Ester Substitution as a Strategy for Optimizing PROTAC Permeability and Cellular Activity

[Image: see text] Criteria for predicting the druglike properties of “beyond Rule of 5” Proteolysis Targeting Chimeras (PROTAC) degraders are underdeveloped. PROTAC components are often combined via amide couplings due to their reliability. Amides, however, can give rise to poor absorption, distribu...

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Detalles Bibliográficos
Autores principales: Klein, Victoria G., Bond, Adam G., Craigon, Conner, Lokey, R. Scott, Ciulli, Alessio
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2021
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8713283/
https://www.ncbi.nlm.nih.gov/pubmed/34881891
http://dx.doi.org/10.1021/acs.jmedchem.1c01496

Internet

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8713283/
https://www.ncbi.nlm.nih.gov/pubmed/34881891
http://dx.doi.org/10.1021/acs.jmedchem.1c01496

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