Fig. 5: MEK1 mutations at the identified regions had different sensitivities to MEK and BRAF inhibitors in cell viability and MAPK pathway signalling assays.
From: The identification of functional regions of MEK1 using CRISPR tiling screens
a Dose response curves of A375 cell line viability in response to selumetinib, trametinib or vemurafenib. The upper panel of curves include the MEK1 activating mutations and the lower panel include the allosteric pocket influencing mutations. Cell viability is shown as percentage to the DMSO control. Data points with three replicates are shown. b MAPK pathway signalling upon selumetinib treatment. Effects of 2 h treatment with 0.1 µM or 10 µM selumetinib on MAPK pathway signalling were tested in the A375 cell lines. c MAPK pathway signalling upon vemurafenib treatment. Effects of 2 h treatment with 0.3 µM or 10 µM vemurafenib on MAPK pathway signalling were tested in the A375 cell lines. DMSO treatment is indicated as ‘-’. Band intensity was quantitated by densitometry. And fold changes of pMEK (S218/S222)/tMEK ratios to the wild-type are indicated below the plots as numbers.
