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Association details:
Biomarker:FLT3 D835V
Cancer:Acute Myelogenous Leukemia
Drug:JQ-1 (BET inhibitor)
Direction:Sensitive
Evidence:
Evidence Level:
Sensitive: D – Preclinical
New
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