Differential transactivation by the androgen receptor in prostate cancer cells

Selectively Targeting the DNA-binding Domain of the Androgen Receptor as a Prospective Therapy for Prostate Cancer

“…Using a luciferase reporter assay in PC3 cells driven by the ARR 3 tk probasin-based promoter (30), two compounds predicted to bind to the AR-DBD showed dose-dependent inhibition of the transiently expressed full-length human AR (Fig. 1C, upper panel, VPC-14228 and VPC-14449, IC 50 ϭ 2.36 and 0.340 M, respectively) without affecting AR protein expression (Fig.…”

Activation of the Androgen Receptor N-terminal Domain by Interleukin-6 via MAPK and STAT3 Signal Transduction Pathways

“…The following plasmids have been described previously: PSA (Ϫ630/ϩ12)-luciferase (28,33,34), PB-luciferase (35), ARR 3 -tk-luciferase (36), AR-(1-558)-Gal4DBD, Gal4DBD (the control vector), and p5ϫGal4UAS-TATA-luciferase (28). AR-(1-233)-Gal4DBD, AR-(234 -390)-Gal4DBD, and AR-(391-558)-Gal4DBD plasmids were constructed by PCR of the nucleotides 363-1062, 1063-1533, 1534 -2037, respectively, of the human AR cDNA using primers 5Ј-AAA AGG ATC CGG ATG GAA GTG CAG TTA GGG CT and 5Ј-TTT GGA TCC TCA GTT GTC AGA AAT GGT CGA AGTBGCC, or 5Ј-AAA AGG ATC CGG GCC AAG GAG TTG TGT AAG GCA GT and 5Ј-AAA AGG CTT CAG GTC TTC TGG GGT GGA AAG TAA TAG as described previously (28).…”

“…The first of these constructs was the probasin (PB)-promoter (Ϫ286/ϩ28) which is a naturally occurring androgen-regulated promoter from the rat that contains ARE1 and ARE2 (35). As shown in Fig.…”

Antagonism between PTEN/MMAC1/TEP-1 and Androgen Receptor in Growth and Apoptosis of Prostatic Cancer Cells

“…To determine whether PTEN also represses endogenous AR activity with natural promoters, we transfected PSALuc into PTEN-null but AR-positive LNCaP cells (22) and examined the effect of PTEN and the PI3K inhibitor on endogenous AR activity. PSALuc is an AR reporter in which luciferase expression is under the control of the promoter of human PSA, a PCa marker, which is transcriptionally regulated by AR through complex AREs (29). As shown in Fig.…”