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. 2019 Aug 20;2(4):e201800213. doi: 10.26508/lsa.201800213

Figure 2. IRC117539 induces AR protein degradation by the proteasome.

Figure 2.

(A) Western blot analysis of AR protein levels in LNCaP, VCaP, and 22Rv1 prostate cancer cells treated with 1 μM IRC117539 compound for indicated times. Note two different AR isoforms (FL, full-length retaining LBD; ΔLBD, the truncated variant) in 22Rv1 cells, which are both degraded. (B) Dose-dependent kinetics of IRC117539-induced AR degradation in LNCaP cells (left panel). AR protein levels were quantified after Western blot and normalized to vinculin (n = 3, representative blots are shown in Figs 2A and S2B). A dose–response graphic for the 24-h time point is shown in the right panel. (C) Proteasome-dependent degradation of AR. Western blot (left) shows AR protein levels in LNCaP cells exposed to 1 μM IRC117539, with or without proteasome inhibition. Right panel shows quantification of AR protein levels at 24 h (n = 3). (D) Western blot analysis of AR protein levels in LNCaP cells co-treated with 10 μM PD169316, a small molecule proteasome activator. Note accelerated kinetics of IRC117539-induced AR degradation. Data information: in (B and C), data are presented as mean ± SEM (n = 3). Asterisks denote statistical significance (*P < 0.05, **P < 0.01, ***P < 0.001, using t test assuming unequal variances).