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

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

Activated RAS promotes dimerization of members of the RAF kinase family1-3. ATP-competitive RAF inhibitors activate ERK signaling4-7 by transactivating RAF dimers4. In melanomas with mutant BRAF(V600E), levels of RAS activation are low and these drugs bind to BRAF(V600E) monomers and inhibit their a...

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Bibliographic Details
Main Authors: 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: Online
Language:English
Published: 2011
Online Access:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3266695/

Internet

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3266695/

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