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Association details:
Biomarker:EZH2 Y641F
Cancer:Melanoma
Drug:Tafinlar (dabrafenib) (BRAF inhibitor)
Direction:Sensitive
Evidence:
Evidence Level:
Sensitive: D – Preclinical
New
Source:
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melanoma with three EZH2 inhibitors: UNC1999 (ref. 36), GSK126 (ref. 37) and a previously unpublished SAM-competitive pyridinone inhibitor, JQEZ5....Ezh2 inhibitors demonstrate anti-neoplastic activity in Ezh2Y641F-mutant cancers.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