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Association details:
| Biomarker: | EZH2 Y641F |
|---|---|
| Cancer: | Melanoma |
| Drug: | UNC1999 (EZH2 inhibitor, EZH1 inhibitor) |
| Direction: | Sensitive |
Evidence:
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melanoma with three EZH2 inhibitors: UNC1999 (ref. 36), GSK126 (ref. 37) and a previously unpublished SAM-competitive pyridinone inhibitor, JQEZ5....Ezh2 inhibitors demonstrate anti-neoplastic activity in Ezh2Y641F-mutant cancers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
