RAF inhibitor resistance is mediated by dimerization of aberrantly spliced BRAF(V600E)

Activated RAS promotes dimerization of members of the RAF kinase family(1-3). ATP-competitive RAF inhibitors activate ERK signaling(4-7) by transactivating RAF dimers(4). In melanomas with mutant BRAF(V600E), levels of RAS activation are low and these drugs bind to BRAF(V600E) monomers and inhibit t...

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Hauptverfasser: Poulikakos, Poulikos I., Persaud, Yogindra, Janakiraman, Manickam, Kong, Xiangju, Ng, Charles, Moriceau, Gatien, Shi, Hubing, Atefi, Mohammad, Titz, Bjoern, Gabay, May Tal, Salton, Maayan, Dahlman, Kimberly B., Tadi, Madhavi, Wargo, Jennifer A., Flaherty, Keith T., Kelley, Mark C., Misteli, Tom, Chapman, Paul B., Sosman, Jeffrey A., Graeber, Thomas G., Ribas, Antoni, Lo, Roger S., Rosen, Neal, Solit, David B.
Format: Artigo
Sprache:Inglês
Veröffentlicht: 2011
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Article
Online Zugang:https://ncbi.nlm.nih.gov/pmc/articles/PMC3266695/
https://ncbi.nlm.nih.gov/pubmed/22113612
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1038/nature10662
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