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Association details:
Biomarker:EZH2 W113C
Cancer:Lymphoma
Drug Class:PRC2 inhibitor
Direction:Sensitive
Evidence:
Evidence Level:
Sensitive: D – Preclinical
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.2023.10307