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Association details:
Biomarker:CEBPA mutation
Cancer:Acute Myelogenous Leukemia
Drug:OICR-9429 (WDR5 inhibitor)
Direction:Sensitive
Evidence:
Evidence Level:
Sensitive: D – Preclinical
New
Title:

Pharmacological targeting of the Wdr5-MLL interaction in C/EBPa N-terminal leukemia

Excerpt:
...we tested whether primary human AML cells with N-terminal C/EBPα mutations would be sensitive to WDR5 antagonism. At 5 μM, OICR-9429 caused a significant decrease in viability in the majority of patient cells with mutations in the N-terminal part of the CEBPA gene (mean viability; 53%, n=8, Fig. 6e). Strikingly, the same concentration of OICR-9429 had little effect on viability in AML patient cells with other mutations (mean viability: 86%, n=5).
DOI:
10.1038/nchembio.1859