• J. Cell Biol. · Oct 2012

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

    • Matthew J Davis and Joseph Schlessinger.
    • Department of Pharmacology, Yale University School of Medicine, New Haven, CT 06520, USA.
    • J. Cell Biol. 2012 Oct 1;199(1):15-9.

    AbstractThe 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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