The genesis of Zelboraf: targeting mutant B-Raf in melanoma

Matthew J Davis, Joseph Schlessinger
Journal of Cell Biology 2012 October 1, 199 (1): 15-9
The protein kinase B-Raf is a critical component of the Ras/MAPK signaling pathway. An oncogenic B-Raf mutation that constitutively activates the kinase was identified in ~50% of melanoma patients and in other cancers. A structure-guided drug discovery approach enabled the development of Zelboraf, a targeted inhibitor of oncogenic B-Raf. This drug has been used successfully in the clinic to treat metastatic melanoma patients harboring B-Raf mutations.

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