Inhibitors of BRAF dimers using an allosteric site

BRAF kinase, a critical effector of the ERK signaling pathway, is hyperactivated in many cancers. Oncogenic BRAF(V600E) 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...

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Udgivet i:Nat Commun
Main Authors: Cotto-Rios, Xiomaris M., Agianian, Bogos, Gitego, Nadege, Zacharioudakis, Emmanouil, Giricz, Orsi, Wu, Yang, Zou, Yiyu, Verma, Amit, Poulikakos, Poulikos I., Gavathiotis, Evripidis
Format: Artigo
Sprog:Inglês
Udgivet: Nature Publishing Group UK 2020
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Article
Online adgang:https://ncbi.nlm.nih.gov/pmc/articles/PMC7462985/
https://ncbi.nlm.nih.gov/pubmed/32873792
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1038/s41467-020-18123-2
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