A selective and orally bioavailable VHL-recruiting PROTAC achieves SMARCA2 degradation in vivo

Targeted protein degradation offers an alternative modality to classical inhibition and holds the promise of addressing previously undruggable targets to provide novel therapeutic options for patients. Heterobifunctional molecules co-recruit a target protein and an E3 ligase, resulting in ubiquityla...

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Detalles Bibliográficos
Autores principales: Kofink, Christiane, Trainor, Nicole, Mair, Barbara, Wöhrle, Simon, Wurm, Melanie, Mischerikow, Nikolai, Roy, Michael J., Bader, Gerd, Greb, Peter, Garavel, Géraldine, Diers, Emelyne, McLennan, Ross, Whitworth, Claire, Vetma, Vesna, Rumpel, Klaus, Scharnweber, Maximilian, Fuchs, Julian E., Gerstberger, Thomas, Cui, Yunhai, Gremel, Gabriela, Chetta, Paolo, Hopf, Stefan, Budano, Nicole, Rinnenthal, Joerg, Gmaschitz, Gerhard, Mayer, Moriz, Koegl, Manfred, Ciulli, Alessio, Weinstabl, Harald, Farnaby, William
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Nature Publishing Group UK 2022
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9551036/
https://www.ncbi.nlm.nih.gov/pubmed/36216795
http://dx.doi.org/10.1038/s41467-022-33430-6

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