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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...
| Autores principales: | , , , , |
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| Formato: | Online Artículo Texto |
| Lenguaje: | English |
| Publicado: |
American Chemical Society
2021
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| 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 |