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

โœ Scribed by Poulikakos, Poulikos I.; Persaud, Yogindra; Janakiraman, Manickam; Kong, Xiangju; Ng, Charles; Moriceau, Gatien; Shi, Hubing; Atefi, Mohammad; Titz, Bjoern; Gabay, May Tal

Book ID
111965086
Publisher
Nature Publishing Group
Year
2011
Tongue
English
Weight
716 KB
Volume
480
Category
Article
ISSN
0028-0836

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RAF inhibitor resistance is mediated by
RAF inhibitor resistance is mediated by dimerization of aberrantly spliced BRAF(V600E)
โœ Poulikakos, Poulikos I.; Persaud, Yogindra; Janakiraman, Manickam; Kong, Xiangju ๐Ÿ“‚ Article ๐Ÿ“… 2011 ๐Ÿ› Nature Publishing Group ๐ŸŒ English โš– 716 KB

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