Development of a covalent cereblon-based PROTAC employing a fluorosulfate warhead

Many cereblon (CRBN) ligands have been used to develop proteolysis targeting chimeras (PROTACs), but all are reversible binders of the E3 ubiquitin ligase. We recently described the use of sulfonyl exchange chemistry to design binders that covalently engage histidine 353 in CRBN for the first time....

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Detalles Bibliográficos
Autores principales: Nowak, Radosław P., Ragosta, Leah, Huerta, Fidel, Liu, Hu, Ficarro, Scott B., Cruite, Justin T., Metivier, Rebecca J., Donovan, Katherine A., Marto, Jarrod A., Fischer, Eric S., Zerfas, Breanna L., Jones, Lyn H.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: RSC 2023
Materias:
Chemistry
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10619143/
https://www.ncbi.nlm.nih.gov/pubmed/37920397
http://dx.doi.org/10.1039/d3cb00103b

Internet

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10619143/
https://www.ncbi.nlm.nih.gov/pubmed/37920397
http://dx.doi.org/10.1039/d3cb00103b

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