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    Association details:
    Biomarker:MAP2K1 Q56P
    Cancer:Melanoma
    Drug:Zelboraf (vemurafenib) (BRAF inhibitor, BRAF V600E inhibitor)
    Direction:Resistant
    Evidence:
    Evidence Level:
    Resistant: C3 – Early Trials
    Source:
    J Clin Oncol
    Title:

    Pharmacodynamic effects and mechanisms of resistance to vemurafenib in patients with metastatic melanoma

    Published date:
    10/04/2013
    Excerpt:
    Acquired resistance to vemurafenib associated with reactivation of MAPK signaling as observed by elevated ERK1/2 phosphorylation levels in progressive lesions and the appearance of secondary NRAS(Q61) mutations or MEK1(Q56P) or MEK1(E203K) mutations.
    DOI:
    10.1200/JCO.2012.44.7888
    Evidence Level:
    Resistant: D – Preclinical
    New
    Source:
    Proc Natl Acad Sci U S A
    Title:

    MEK1 mutations confer resistance to MEK and B-RAF inhibition

    Excerpt:
    Both MEK1(P124L) and MEK1(Q56P), which disrupts helix A, conferred cross-resistance to PLX4720, a selective B-RAF inhibitor in A375 cells.
    DOI:
    10.1073/pnas.0905833106