FIGURE 1. The BRAF(V600E) mutation confers sensitivity to the MEK inhibitor CI-1040.
From the following article:
BRAF mutation predicts sensitivity to MEK inhibition
David B. Solit, Levi A. Garraway, Christine A. Pratilas, Ayana Sawai, Gad Getz, Andrea Basso, Qing Ye, Jose M. Lobo, Yuhong She, Iman Osman, Todd R. Golub, Judith Sebolt-Leopold, William R. Sellers & Neal Rosen
Nature 439, 358-362(19 January 2006)
doi:10.1038/nature04304
a, CI-1040 IC50 values as a function of BRAF and NRAS mutational status. b, Immunoblot of p-ERK and total ERK, demonstrating that CI-1040 inhibits MAPK activity with IC50 values ranging from 100 to 500 nM. Cells were treated for 24 h. MEK inhibition caused profound downregulation of cyclin D1 expression in BRAF mutant tumour cells. In contrast, cyclin D1 declined only modestly in SKMEL103 melanoma cells with the NRAS(Q61R) mutation and in SKMEL31 RAS/BRAF-WT cells. Cyclin D1 expression was unaffected by CI-1040 in non-melanoma cells with wild-type RAS and BRAF.
