Fig. 7

Impact of ARTADIs on AR protein-protein interactions. a AR RIME was performed in androgen-stimulated (+) LNCaP cells treated with DMSO vehicle, enzalutamide (5 µM), EPI-002/ralaniten (35 µM) or BU3-12 (5 µM). Average peptide coverage of AR bait protein for each treatment (n = 2). b A CirGO image plot of clustered gene ontology terms (molecular function) which were associated with AR interactions in vehicle treated samples stimulated with R1881. c PCA plot based upon 97 AR-specific interactions. d Radar chart showing top AR-binding partners in vehicle treated samples stimulated with R1881. Members of the SWI-SNF chromatin remodeling complex (blue) and known AR co-regulatory partners (red) are shown. e Heatmap showing selected AR-interactions following treatment with inhibitors. f Cartoon showing proposed model of ARTADI and enzalutamide antagonism of AR coregulatory proteins. g Plots showing AR interactions using PLA and normalized to vehicle control. LNCaP cells were pretreated with vehicle, ENZA (5 µM), EPI-7386 (5 µM), BU170 (10 µM), BU3-12 (5 µM), or normal rabbit and mouse IgG for 1 h and stimulated with R1881 (1 nM) for 2 h. h Plots showing AR-V7 interactions using PLA and normalized to vehicle control. VCaP-ENZR cells were treated with vehicle, ENZA (5 µM), EPI-7386 (5 µM), BU170 (10 µM), BU3-12 (5 µM) or normal rabbit and mouse IgG for 3 h. Bars represented the mean ± SEM (n = 3–6 independent experiments). *p < 0.05, **p < 0.01, ***p < 0.001, ****p < 0.0001. See Supplementary Fig. 6