Article
Melanomas acquire resistance to B-RAF(V600E) inhibition by RTK or N-RAS upregulation.
Nature - 16 Dec 2010
Nazarian Ramin, Shi Hubing, Wang Qi, Kong Xiangju, Koya Richard C, Lee Hane, Chen Zugen, Lee Mi-Kyung, Attar Narsis, Sazegar Hooman, Chodon Thinle, Nelson Stanley F, McArthur Grant, Sosman Jeffrey A, Ribas Antoni, Lo Roger S
Abstract excerpt
Activating B-RAF(V600E) (also known as BRAF) kinase mutations occur in ∼7% of human malignancies and ∼60% of melanomas. Early clinical experience with a novel class I RAF-selective inhibitor, PLX4032, demonstrated an unprecedented 80% anti-tumour response rate among patients with B-RAF(V600E)-positive melanomas, but acquired drug resistance frequently develops after initial responses. Hypotheses for mechanisms of...
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