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Association details:
| Biomarker: | EZH2 W113C |
|---|---|
| Cancer: | Lymphoma |
| Drug: | Tazverik (tazemetostat) (EZH2 inhibitor) |
| Direction: | Resistant |
Evidence:
Source:
Title:
EZH2 W113C is a gain-of-function mutation in B-cell lymphoma enabling both PRC2 methyltransferase activation and tazemetostat resistance
Published date:
02/27/2023
Excerpt:
Intriguingly, the W113C mutation leads to tazemetostat resistance in both H3K27 methylation and tumor proliferation. Another class of allosteric PRC2 inhibitor binding EED overcomes the resistance, effectively decreases H3K27me3, and blocks tumor proliferation in cells expressing EZH2 W113C.
DOI:
10.1016/j.jbc.2023.103073
