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    BIOMARKER:

    MAP2K1 S222D

    i
    Other names: MAP2K1, MAPKK1, MEK1, PRKMK1, Mitogen-activated protein kinase kinase 1
    Entrez ID:
    5604
    Related biomarkers:
    Expression
    Mutation
    CNA
    Others
    Associations

    News

    Trials
    over3years
    Allosteric Kinase Inhibitors Reshape MEK1 Kinase Activity Conformations in Cells and In Silico. (PubMed, Biomolecules)
    Application of the allosterically acting MEK inhibitors (MEKi) trametinib, cobimentinib, refametinib, and selumetinib converted activated MEK1 KinCon reporters back into a more closed inactive conformation. We observed increased dynamics for the S218D/S222D double mutant particularly in the region of the distal A-helix and alpha-C helix. These data underline that MEK1 KinCon biosensors have the potential to be subjected to MEKi efficacy validations in an intact cell setting.
    Journal
    |
    BRAF (B-raf proto-oncogene) • MAP2K1 (Mitogen-activated protein kinase kinase 1)
    |
    BRAF V600E • BRAF V600 • MAP2K1 mutation • MAP2K1 S218D • MAP2K1 S222D
    |
    Mekinist (trametinib) • Koselugo (selumetinib) • refametinib (BAY86-9766)