Fig. 3

LSD1 chemical inhibition depletes AR response element activation through the AR-V7 splice variant. Luciferase reporter assay of AR response element (ARE) promotor activation in HEK293 cells co-transfected, 24 h after seeding as indicated, with either AR-WT or AR-V7 expression vectors, and incubated 24 h later as indicated with dihydrotestosterone (DHT, 1 nM), LSD1-C76 (250 μM) or HCl-2509 (5 μM) or DMSO solvent control and then analysed at 18 h. Samples were normalized against the AR-WT DMSO treated samples. Data are mean values ± standard deviation from 4 separate experiments each with triplicate determinations. P values were derived using a two-way ANOVA for comparison followed by Tukey’s multiple comparison post hoc tests. AR androgen receptor; WT wild type; ****P < 0.0001