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Cell‐Based Optimization of Covalent Reversible Ketoamide Inhibitors Bridging the Unprimed to the Primed Site of the Proteasome β5 Subunit

The ubiquitin‐proteasome system (UPS) is an established therapeutic target for approved drugs to treat selected hematologic malignancies. While drug discovery targeting the UPS focuses on irreversibly binding epoxyketones and slowly‐reversibly binding boronates, optimization of novel covalent‐revers...

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Detalles Bibliográficos
Autores principales: Stubba, Daniel, Bensinger, Dennis, Steinbacher, Janika, Proskurjakov, Lilia, Salcedo Gómez, Álvaro, Schmidt, Uwe, Roth, Stefan, Schmitz, Katja, Schmidt, Boris
Formato: Online Artículo Texto
Lenguaje:English
Publicado: John Wiley and Sons Inc. 2019
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6916368/
https://www.ncbi.nlm.nih.gov/pubmed/31675179
http://dx.doi.org/10.1002/cmdc.201900472