How to fool a wonder drug: truncate and dimerize

Cancer Cell. 2012 Jan 17;21(1):7-9. doi: 10.1016/j.ccr.2011.12.017.

Abstract

In a recent paper, Poulikakos et al. describe a new and potentially common mechanism whereby melanomas develop resistance to the BRAF inhibitor vemurafenib by expressing truncated forms of BRAF(V600E) that can dimerize in the absence of activated RAS. Will it be possible to block this with improved BRAF inhibitor design?

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