Article
Identification of a novel family of BRAF(V600E) inhibitors.
Journal of medicinal chemistry - 14 Jun 2012
Qin Jie, Xie Peng, Ventocilla Christian, Zhou Guoqiang, Vultur Adina, Chen Quan, Liu Qin, Herlyn Meenhard, Winkler Jeffrey, Marmorstein Ronen
Abstract excerpt
The BRAF oncoprotein is mutated in about half of malignant melanomas and other cancers, and a kinase activating single valine to glutamate substitution at residue 600 (BRAF(V600E)) accounts for over 90% of BRAF-mediated cancers. Several BRAF(V600E) inhibitors have been developed, although they harbor some liabilities, thus motivating the development of other BRAF(V600E) inhibitor options. We report here the use...
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