background: androgen insensitivity syndrome (ais) or testicular feminization is a partial or complete inability of cell response to androgen. the cause is enzymatic defect in synthesis of testosterone, resulting sexually immature phenotypically female, with primary amenorrhea. there are three categories of ais, complete, partial and mild, depending on the degree of external genital masculinizat...

Autoregulation is a control mechanism common to several proteins of the steroid/thyroid hormone receptor superfamily. In this work, the effect of androgens and antiandrogens on the expression of the human androgen receptor (hAR) in prostate and breast cancer cell lines was studied. Northern blot analysis revealed a decrease in hAR steady state RNA levels in LNCaP cells by 3.3 nM of the syntheti...

The growth and development of the prostate gland are regulated by the androgen and the androgen receptor (AR). Despite our molecular understanding of the roles of the AR regulating; a downstream target gene transcription, the direct or indirect (stromally mediated) actions of the androgen in controlling prostate cell growth and differentiation are still unclear. In this report, an invasive; and...

Spinal and bulbar muscular atrophy (SBMA) is an X-linked, adult-onset, neurodegenerative disorder affecting only males and is caused by expanded polyglutamine (polyQ) stretches in the N-terminal A/B domain of human androgen receptor (hAR). Although no overt phenotype was detected in adult fly eye photoreceptor neurons expressing mutant hAR (polyQ 52), ingestion of androgen or its known antagoni...

BACKGROUND Prostate cancer is the leading tumor of the male in Western societies. Genetic alterations of the androgen receptor gene are known in the advanced metastatic disease. In this study, the androgen receptor gene was tested in two human prostate cancer cell lines, the androgen-sensitive PC-EW and the androgen-independent PC-OR. MATERIALS AND METHODS Genomic DNA was isolated from two ce...

The health effects of perfluorooctanoic acid (PFOA) on humans remain controversial because of contradictory experimental and epidemiological studies. In this study, we used three-dimensional quantitative structure-activity relationship (3D-QSAR) method by applying Surflex-dock to study the binding modes between PFOA and human estrogen receptor (hERα), human androgen receptor (hAR) and human thy...

We produced polyclonal antibody against human androgen receptor (hAR) by means of immunizing a rabbit with hAR fusion protein that was expressed in E. coli. In Western blot analysis, this antibody, NH27, recognized two protein bands at the site of 110 kDa and 107 kDa in androgen-independent human prostatic cancer cells (PC-3), transfected with full-length hAR expression plasmid DNA and at the s...

In humans, spironolactone and mespirenone are well known antimineralocorticoids without C-11beta substituents. These compounds display antagonist properties by acting through the human androgen receptor (hAR). In contrast, we demonstrate here that synthetic mineralocorticoid antagonists bearing hydrophobic C-11beta substituents and C-17gamma-lactone are potent hAR agonists in vitro. The three-d...

In humans, spironolactone and mespirenone are well known antimineralocorticoids without C-11b substituents. These compounds display antagonist properties by acting through the human androgen receptor (hAR). In contrast, we demonstrate here that synthetic mineralocorticoid antagonists bearing hydrophobic C-11b substituents and C-17g-lactone are potent hAR agonists in vitro. The three-dimensional...

Antiandrogenic chemicals alter sex differentiation by several different mechanisms. Some, like flutamide, procymidone, or vinclozolin compete with androgens for the androgen receptor (AR), inhibit AR-DNA binding, and alter androgen-dependent gene expression in vivo and in vitro. Finasteride and some phthalate esters demasculinize male rats by inhibiting fetal androgen synthesis. Linuron, which ...