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Association details:
Biomarker:EZH2 mutation
Cancer:Diffuse Large B Cell Lymphoma
Drug Class:USP47 inhibitor
Direction:Sensitive
Evidence:
Evidence Level:
Sensitive: D – Preclinical
Source:
Title:

Inhibition of the deubiquitinating enzyme USP47 as a novel targeted therapy for hematologic malignancies expressing mutant EZH2

Published date:
01/17/2022
Excerpt:
Inhibition of USP47 would be anticipated to block the function of mutated EZH2 through induction of EZH2 degradation by promoting its ubiquitination. Moreover, targeting of USP47 leads to death of mutant EZH2-positive cells in vitro and in vivo. Taken together, we propose targeting USP47 with a small molecule inhibitor as a novel potential therapy for DLBCL and other hematologic malignancies characterized by mutant EZH2 expression.
DOI:
10.1038/s41375-021-01494-w