Discovery of DDO-2213 as a Potent and Orally Bioavailable Inhibitor of the WDR5–Mixed Lineage Leukemia 1 Protein–Protein Interaction for the Treatment of MLL Fusion Leukemia

Abstract excerpt

WD repeat-containing protein 5 (WDR5) is essential for the stability and methyltransferase activity of the mixed lineage leukemia 1 (MLL1) complex. Dysregulation of the MLL1 gene is associated with human acute leukemias, and the direct disruption of the WDR5–MLL1 protein–protein interaction (PPI) is emerging as an alternative strategy for MLL-rearranged cancers. Here, we represent a new aniline pyrimidine...

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