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    Association details:
    Biomarker:FLT3 F691L
    Cancer:Acute Myelogenous Leukemia
    Drug:JQ-1 (BET inhibitor)
    Direction:Sensitive
    Evidence:
    Evidence Level:
    Sensitive: D – Preclinical
    New
    Source:
    Mol Cancer Ther
    Title:

    BET Protein Antagonist JQ1 Is Synergistically Lethal with FLT3 Tyrosine Kinase Inhibitor (TKI) and Overcomes Resistance to FLT3-TKI in AML Cells Expressing FLT-ITD

    Excerpt:
    JQ1-induced apoptosis in the BaF3 cells expressing FLT3-ITD, FLT3-ITD-F691L, and FLT3-ITD-D835V was associated with JQ1-mediated attenuation of c-MYC, but induction of HEXIM1 and BIM (the extra-long, long, and short isoforms; Fig. 4B). Thus, JQ1 retains effectiveness against cells expressing the clinically encountered mutations in FLT3 that confer resistance to FLT3-TKI.
    DOI:
    10.1158/1535-7163.MCT-14-0258