Figure 4. CLA-9Z11E inhibits AR coactivator interaction and PSA expression.
AR Coactivator Interaction Assay in A) antagonist and B) agonist models were performed to test the ability of CLA-9Z11E to affect coactivator peptide recruitment and binding to AR. Cyproterone acetate (IC50: 672 nM) was used as a positive control for the antagonist assay and R1881, a synthetic AR agonist, was used for the agonist assay. Data are expressed as mean ± standard deviation of duplicate assays. LNCaP and VCaP cells were treated by 1 nM DHT with CLA-9Z11E (10 μM~500 μM) for 48h. AR reporter activity in C) LNCaP and D) VCaP cells was determined by PSA promoter-luciferase assay. The mRNA levels of AR and PSA in E) LNCaP and F) VCaP cells was quantified by qRT-PCR. The results are expressed as mean ± standard deviation of three independent experiments, p values were determined by multiple Student's t-tests. *p<0.05, **p<0.01, ***p<0.001. ns. No significant difference.