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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Auteurs principaux: 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
Langue:Inglês
Publié: 2011
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Article
Accès en ligne: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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