...Frazer A. Cook; Simon J. Cook The RAS-regulated RAF–MEK1/2–ERK1/2 pathway promotes cell proliferation and survival and RAS and BRAF proteins are commonly mutated in cancer. This has fuelled the development of small molecule kinase inhibitors including ATP-competitive RAF inhibitors. Type I and type...

...Pablo G. Jambrina; Olga Bohuszewicz; Nicolae-Viorel Buchete; Walter Kolch; Edina Rosta Protein phosphorylation is one of the most common post-translational modifications in cell regulatory mechanisms. Dimerization plays also a crucial role in the kinase activity of many kinases, including RAF, CDK2...

... by the adenine ring of ATP. In the present paper, we show how the spine concept can be applied to B-Raf, specifically to engineer a kinase-dead pseudokinase. To achieve this, we mutated one of the C-spine residues in the N-lobe (N-terminal lobe), Ala 481 , to phenylalanine. This mutant cannot bind ATP...

... (Her3) kinase suppressor of Ras (KSR) mitogen-activated protein kinase (MAPK) extracellular-signal-regulated kinase pseudokinase Raf © The Authors Journal compilation © 2013 Biochemical Society 2013 11 6 2013 1 email [email protected] CASK is only one example where...

... cues. This has been particularly elucidated for the Ras/Raf/MEK [mitogen-activated growth factor/ERK (extracellular-signal-regulated kinase) kinase]/ERK signalling pathway with a number of studies in fibroblasts showing that sustained ERK signalling is a requirement for S-phase entry, whereas transient...