Article
Inhibitors of BRAF dimers using an allosteric site.
Nature communications - 1 Sept 2020
Cotto-Rios Xiomaris M, Agianian Bogos, Gitego Nadege, Zacharioudakis Emmanouil, Giricz Orsi, Wu Yang, Zou Yiyu, Verma Amit, Poulikakos Poulikos I, Gavathiotis Evripidis
Abstract excerpt
BRAF kinase, a critical effector of the ERK signaling pathway, is hyperactivated in many cancers. Oncogenic BRAFV600E signals as an active monomer in the absence of active RAS, however, in many tumors BRAF dimers mediate ERK signaling. FDA-approved RAF inhibitors poorly inhibit BRAF dimers, which leads to tumor resistance. We found that Ponatinib, an FDA-approved drug, is an effective inhibitor of BRAF monomers...
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