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    BIOMARKER:

    MAP2K1 V211D

    i
    Other names: MAP2K1, MAPKK1, MEK1, PRKMK1, Mitogen-activated protein kinase kinase 1
    Entrez ID:
    5604
    Related biomarkers:
    Expression
    Mutation
    CNA
    Others
    over4years
    V211D mutation in MEK1 causes resistance to MEK inhibitors in colon cancer. (PubMed, Cancer Discov)
    We report the emergence of the novel MEK1 gatekeeper mutation in a patient with BRAF colon cancer treated with the allosteric MEK inhibitor binimetinib and the anti-EGFR antibody panitumumab. Moreover, the mutant exhibits reduced sensitivity to all the allosteric MEK inhibitors tested. Thus this mutation serves as a general resistance mutation for current MEK inhibitors; however, it is sensitive to a newly reported ATP-competitive MEK inhibitor, which therefore could be used to overcome drug resistance.
    Journal
    |
    BRAF (B-raf proto-oncogene) • MAP2K1 (Mitogen-activated protein kinase kinase 1)
    |
    BRAF mutation • MAP2K1 mutation • MAP2K1 V211D
    |
    Vectibix (panitumumab) • Mektovi (binimetinib)