Article
Identification of type II inhibitors targeting BRAF using privileged pharmacophores.
Chemical biology & drug design - 1 Jan 2014
Zhang Qingwen, Wang Juan, Wang Fei, Chen Xiuhua, He Yunsong, You Qidong, Zhou Houyuan
Abstract excerpt
V-RAF murine sarcoma viral oncogene homologue B1 (BRAF) is the most frequently mutated protein kinase in human cancers. The most common mutant BRAF V600E constitutively activates the RAS/RAF/MEK/ERK signaling pathway. BRAF has been validated as an important therapeutic target in human cancers. Phenylaminopyrimidine and unsymmetrical diaryl urea are two privileged pharmacophores in kinase inhibitor drug discovery....
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