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Leukemia-specific delivery of mutant NOTCH1 targeted therapy #MMPMID29158376
Roti G; Qi J; Kitara S; Sanchez-Martin M; Saur Conway A; Varca AC; Su A; Wu L; Kung AL; Ferrando AA; Bradner JE; Stegmaier K
J Exp Med 2018[Jan]; 215 (1): 197-216 PMID29158376show ga
NOTCH1 is an attractive cancer target, particularly in T cell acute lymphoblastic leukemia (T-ALL), with activating mutations in this gene identified in more than 50% of cases. In this study, Roti et al. describe the synthesis, characterization, and validation of JQ-FT, a first-in-class NOTCH1 inhibitor that has dual selectivity for leukemia over normal cells and NOTCH1 mutants over wild-type receptors.