Article
Mutation that blocks ATP binding creates a pseudokinase stabilizing the scaffolding function of kinase suppressor of Ras, CRAF and BRAF.
Proceedings of the National Academy of Sciences of the United States of America - 12 Apr 2011
Hu Jiancheng, Yu Haiyang, Kornev Alexandr P, Zhao Jianping, Filbert Erin L, Taylor Susan S, Shaw Andrey S
Abstract excerpt
Because mutations in RAS and BRAF represent the most common mutations found in human tumors, identification of inhibitors has been a major goal. Surprisingly, new oncogenic BRAF specific inhibitors inhibit cells transformed with mutated BRAF but paradoxically stimulate the growth of cells transformed with RAS. Here, we show that the mechanism for activation is via drug-induced dimer formation between CRAF and...
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