Androgen receptor level increases upon small molecule antagonism. (A) AR mRNA expression in VCaP cells (vehicle control and Compound 30, 10 μM) from four microarray probesets (The SAM q-value of differential expression are 0, 0.037, 0.043 and 0.056 respectively). The profiling experiment was performed using three independent biological replicates. (B) AR expression in tumors derived from VCaP cells implanted in CB17/lcr-Prkdc SCID mice and treated with Compounds 26 and 30 as measured by quantitative RT-PCR. n = number of animals per group; mpk = milligram per kilogram. Compound 26- and 30-treated groups were significantly different from Vehicle-group (###, *** P < 0.001). (C) AR expression in VCaP cells treated in triplicate for 48 hr with 25 nM of either control/non-targeted siRNA (Neg-siRNA, Dharmacon Cat# D-001810-10) or AR-siRNA pool (Dharmacon Cat# L-003400-00) as measured by quantitative RT-PCR. AR-siRNA treated samples were significantly different from control/non-targeted ones (P = 3.49e-5).