INDICATION: Chronic lymphocytic leukemia (CLL)
Patient sample, in vitro and mouse studies identified a BRD4 inhibitor that could help treat CLL. In B cells isolated from patients, BRD4 levels were higher than in B cells from healthy volunteers. Screening of BET bromodomain protein inhibitor tool compounds via in vitro binding assays, followed by optimization of a dimethylisoxazole-azaindole-based screening hit, yielded a compound that bound the bromodomain...