Article
Investigation into the Use of Encorafenib to Develop Potential PROTACs Directed against BRAFV600E Protein.
Molecules (Basel, Switzerland) - 3 Dec 2022
Marini Elisabetta, Marino Marco, Gionfriddo Giulia, Maione Federica, Pandini Marta, Oddo Daniele, Giorgis Marta, Rolando Barbara, Blua Federica, Gastaldi Simone, Marchiò Serena, Kovachka Sandra, Spyrakis Francesca, Gianquinto Eleonora, Di Nicolantonio Federica, Bertinaria Massimo
Abstract excerpt
BRAF is a serine/threonine kinase frequently mutated in human cancers. BRAFV600E mutated protein is targeted through the use of kinase inhibitors which are approved for the treatment of melanoma; however, their long-term efficacy is hampered by resistance mechanisms. The PROTAC-induced degradation of BRAFV600E has been proposed as an alternative strategy to avoid the onset of resistance. In this study, we...
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