Encoding BRAF inhibitor functions in protein degraders?
RSC Medicinal Chemistry Pub Date: 2022-05-05 DOI: 10.1039/D2MD00064D
Abstract
Various BRAF kinase inhibitors were developed to treat cancers carrying the BRAFV600E mutation. First-generation BRAF inhibitors could lead to paradoxical activation of the MAPK pathway, limiting their clinical usefulness. Here, we show the development of two series of BRAFV600E-targeting PROTACs and demonstrate that the exchange of the inhibitor scaffold from vemurafenib to paradox-breaker ligands resulted in BRAFV600E degraders that did not cause paradoxical ERK activation.
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Journal Name：RSC Medicinal Chemistry
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CAS no.: 89640-58-4
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