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162 Resistance to RAF Inhibitors Due to RAS-independent Dimerization of BRAF(V600E) Splicing Variants

โœ Scribed by Poulikakos, P.I.; Persaud, Y.; Janakiraman, M.; Gabay, M.T.; Dahlman, K.B.; Sosman, J.A.; Ribas, A.; Lo, R.S.; Rosen, N.; Solit, D.B.


Book ID
122975292
Publisher
Elsevier Science
Year
2012
Tongue
English
Weight
73 KB
Volume
48
Category
Article
ISSN
0959-8049

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RAF inhibitor resistance is mediated by
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