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Therapeutics

Iterations of BRAF

Nature Reviews Cancer volume 12, page 374 (2012)Cite this article

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The authors found that MEK phosphorylation was substantially reduced when BRAF DIF mutants were expressed in Plat-E cells. Similarly, the BRAF-E586K tumour-associated mutant, which increases homodimerization, was sensitive to the introduction of DIF mutations. However, the cancer-associated mutants BRAF-V600E, BRAF-G469A and BRAF-insT retained substantial activity when the DIF was mutated despite the fact that DIF mutations reduced homodimerization and formation of large complexes by BRAF-V600E.

BRAF inhibitors ... abrogated the phosphorylation of MEK and ERK when the BRAF DIF was mutated.

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ORIGINAL RESEARCH PAPER

  1. Röring, M. et al. Distinct requirement for an intact dimer interface in wild-type, V600E and kinase-dead B-Raf signalling. EMBO J. 17 Apr 2012 (doi:10.1038/emboj.2012.100)

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  1. Gemma K. Alderton
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Alderton, G. Iterations of BRAF. Nat Rev Cancer 12, 374 (2012). https://doi.org/10.1038/nrc3284

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