While all three coactivators ARA70, steroid receptor coactivator 1, and RAC3/ACTR can enhance androgen receptor (AR) transcriptional activity at 1 nM dihydrotestosterone, we here demonstrate that only ARA70 can induce AR transcriptional activity >30-fold in the presence of 10 nM 17beta-estradiol (E2), but not diethylstilbestrol. The significance of this newly described E2-induced AR transcripti...

17 beta-estradiol enchances androgen-induced prostate growth in the castrate dog to a degree comparable to that seen in spontaneous prostatic hypertrophy. To investigate the mechanism of this synergism, cytosol androgen binding was measured by a density gradient technique in prostates of control and 17 beta-estradiol-treated castrate dogs. [3H]Dihydrotestosterone was bound principally to a moie...

A method has been developed for the simultaneous determination of testosterone, 5alpha-dihydrotestosterone and corticosterone, or of estrone, estradiol-17beta and corticosterone, after separation on a Celite:propylene glycol:ethylene glycol column (6:1.5:1.5 w/v/v). The lower quarter of the column was packed with a Celite: water mixture (3:1 w/v) as a stationary phase (glycol) 'trap'. This eff...

Total plasma androgens (PA) were measured in 9 hypogonadal males aged between 13 and 21 1/2 years after a single oral dose of testosterone undecanoate (TU). With the exception of one patient, all showed a rise in PA with peak values between 7.7 and 38.0 nmol/l at 2 to 7 hours. A further patient aged 15.7 years who was given an 80-mg dose had a peak PA level of 71.2 nmol/l. In all patients PA re...

In vitro models of normal and malignant human prostate are currently limited to a few well established cell lines that, with a single exception (LNCaP), fail to express the androgen receptor (AR) - a common characteristic of prostatic epithelium grown in culture. To investigate the molecular mechanism of action of the non-steroidal antiandrogen Casodex (bicalutamide) against wild-type AR, we ha...

The neural control of the clasp reflex in male Xenopus laevis has been studied by using anatomical, electrophysiological, and biochemical techniques. Neurons in spinal segment 2 of castrated males accumulate label after injection of [3H]-dihydrotestosterone; these neurons are distributed within the rostral portions of the motoneuronal pools of the sternoradialis and flexor carpi radialis muscle...

Using the synthetic androtfen R1881 (17/S-hydroxy-17a-methyl-estra-4,9,ll-trien-3-one) as probe, we identified cytoplasmic androgen receptors in baboon myocardium. The relative binding affinity of selected steroids for the androgen receptor was R1881, 100%; Sa-dihydrotestosterone, 32.8%; testosterone, 29.6%, progesterone, 7.2%; R5020, 1.0%; and estradiol-17/3, 5.8%. The androgen receptor migrat...

The structures of the ligand-binding domains (LBD) of the wild-type androgen receptor (AR) and the T877A mutant corresponding to that in LNCaP cells, both bound to dihydrotestosterone, have been refined at 2.0 A resolution. In contrast to the homodimer seen in the retinoid-X receptor and estrogen receptor LBD structures, the AR LBD is monomeric, possibly because of the extended C terminus of AR...

The intranuclear binding of radioactive hormone in prostate after the intravenous administration of testosterone-l ,2-3H to rats has been studied. Nuclei obtained by sucrose density gradient centrifugation were extracted with buffer containing 0.6 M NaCl, and the soluble radioactivity was separated into bound and free fractions by gel filtration on Sephadex G-25 or G-ZOO. As early as 15 min aft...