Targeting BRAF

    • Rapidly accelerated fibrosarcoma (RAF) kinase family is serine/threonine-specific protein kinases that mediate signal transduction in MAPK pathway. Raf kinases family consists of three isoforms: RAF-1/CRAF, BRAF, ARAF.
    • All Raf proteins share MEK1/2 kinases as a substrate.
    • CRAF overexpression is found in a variety of primary human cancers: lung, liver, prostate, neuroendocrine tumors, and myeloid leukemia.
    • BRAF mutations are found in melanoma (30%–60%), thyroid cancer (30%–50%), colorectal cancer (5%–20%).
    • The most common BRAF mutation, valine (V) is substituted for by glutamate (E) at codon 600 (now referred to as V600E) in the F mutations that are seen in human cancers. BRAF V600E mutation indicates poor prognosis in colorectal cancers.
    Other topics in Molecular Targets and Pathways