Development of a novel class of B-Raf v600e-selective inhibitors through virtual screening and hierarchical hit optimization

…, Z Liang, M Zheng, W Zhu, H Jiang, M Herlyn…

文献索引：Kong, Xiangqian; Qin, Jie; Li, Zeng; Vultur, Adina; Tong, Linjiang; Feng, Enguang; Rajan, Geena; Liu, Shien; Lu, Junyan; Liang, Zhongjie; Zheng, Mingyue; Zhu, Weiliang; Jiang, Hualiang; Herlyn, Meenhard; Liu, Hong; Marmorstein, Ronen; Luo, Cheng Organic and Biomolecular Chemistry, 2012 , vol. 10, # 36 p. 7402 - 7417

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被引用次数: 10

摘要

Oncogenic mutations in critical nodes of cellular signaling pathways have been associated with tumorigenesis and progression. The B-Raf protein kinase, a key hub in the canonical MAPK signaling cascade, is mutated in a broad range of human cancers and especially in malignant melanoma. The most prevalent B-RafV600E mutant exhibits elevated kinase activity and results in constitutive activation of the MAPK pathway, thus making it a ...