Article
The RAF inhibitor PLX4032 inhibits ERK signaling and tumor cell proliferation in a V600E BRAF-selective manner.
Proceedings of the National Academy of Sciences of the United States of America - 17 Aug 2010
Joseph Eric W, Pratilas Christine A, Poulikakos Poulikos I, Tadi Madhavi, Wang Weiqing, Taylor Barry S, Halilovic Ensar, Persaud Yogindra, Xing Feng, Viale Agnes, Tsai James, Chapman Paul B, Bollag Gideon, Solit David B, Rosen Neal
Abstract excerpt
Tumors with mutant BRAF and some with mutant RAS are dependent upon ERK signaling for proliferation, and their growth is suppressed by MAPK/ERK kinase (MEK) inhibitors. In contrast, tumor cells with human EGF receptor (HER) kinase activation proliferate in a MEK-independent manner. These findings have led to the development of RAF and MEK inhibitors as anticancer agents. Like MEK inhibitors, the RAF inhibitor...
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