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    Association details:
    Biomarker:EZH2 Y641F
    Cancer:Melanoma
    Drug:GSK2816126 (EZH2 inhibitor)
    Direction:Sensitive
    Evidence:
    Evidence Level:
    Sensitive: D – Preclinical
    New
    Source:
    Nat Med
    Title:

    An oncogenic Ezh2 mutation cooperates with particular genetic alterations to induce tumors in mice and redistributes H3K27 trimethylation throughout the genome

    Excerpt:
    We treated cell lines derived from TyrCREERT2B-RafV600Ezh2Y641F/+ melanoma with three EZH2 inhibitors: UNC1999 (ref. 36), GSK126 (ref. 37) and a previously unpublished SAM-competitive pyridinone inhibitor, JQEZ5....Ezh2 inhibitors demonstrate anti-neoplastic activity in Ezh2Y641F-mutant cancers.
    DOI:
    10.1038/nm.4092