Article
Tumours with class 3 BRAF mutants are sensitive to the inhibition of activated RAS.
Nature - 10 Aug 2017
Yao Zhan, Yaeger Rona, Rodrik-Outmezguine Vanessa S, Tao Anthony, Torres Neilawattie M, Chang Matthew T, Drosten Matthias, Zhao Huiyong, Cecchi Fabiola, Hembrough Todd, Michels Judith, Baumert Hervé, Miles Linde, Campbell Naomi M, de Stanchina Elisa, Solit David B, Barbacid Mariano, Taylor Barry S, Rosen Neal
Abstract excerpt
Approximately 200 BRAF mutant alleles have been identified in human tumours. Activating BRAF mutants cause feedback inhibition of GTP-bound RAS, are RAS-independent and signal either as active monomers (class 1) or constitutively active dimers (class 2). Here we characterize a third class of BRAF mutants-those that have impaired kinase activity or are kinase-dead. These mutants are sensitive to ERK-mediated...
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