Aromatase is a cytochrome P-450 enzyme complex that catalyzes the conversion of androst-4-ene-3,17-dione (AD) to estrone through three sequential oxygenations of the 19-methyl group. To gain insight into the ability of AD isomers, 4-en-6-one 1a, 5-en-4-one 2a, and 5-en-7-one 3a, competitive inhibitors of aromatase with an A, B-ring enone structure to serve as a substrate, we incubated the three...

1 Jones JS. Saturation biopsy for detecting and characterizing prostate cancer. BJU Int 2007; 99 : 1340–4 2 Mitra AV, EK Bancroft, RA Eeles. A review of targeted screening for prostate cancer: introducing the IMPACT study. BJU Int 2007; 99 : 1350–5 3 Pitts WR. Validation of the Pitts unified theory of prostate cancer, late-onset hypogonadism and carcinoma: the role of steroid 5 α -reductase and...

This review highlights recent studies of the anatomical and functional implications of brain aromatase (estrogen synthase) expression in two vertebrate lineages, teleost fishes and songbirds, that show remarkably high levels of adult brain aromatase activity, protein and gene expression compared to other vertebrate groups. Teleosts and birds have proven to be important neuroethological models f...

The extragonadal synthesis of biological active steroid hormones from their inactive precursors in target tissues is named "intracrinology." Of particular importance for the progression of estrogen-dependent cancers is the in situ formation of the biological most active estrogen, 17beta-estradiol (E2). In cancer cells, conversion of inactive steroid hormone precursors to E2 is accomplished from...

The triazine herbicide atrazine has been hypothesized to disrupt sexual development in frogs by up-regulating aromatase activity, resulting in greater estradiol (E2) concentrations and causing feminization in males. The goal of this study was to collect native ranid frogs from atrazine-exposed ponds and determine whether relationships exist between measured atrazine concentrations and the gonad...

BACKGROUND Endocrine therapy constitutes a central modality in the treatment of oestrogen receptor (ER)-positive advanced breast cancer. PURPOSE To evaluate the evidence for endocrine treatment in postmenopausal patients with advanced breast cancer focusing on the aromatase inhibitors, letrozole, anastrozole, exemestane and fulvestrant. METHODS A review was carried out using PubMed. Randomi...

Inhibition of aromatase is an efficient approach for the prevention and treatment of breast cancer. New A,D-ring modified steroid analogues of formestane and testolactone were designed and synthesized and their biochemical activity was investigated in vitro in an attempt to find new aromatase inhibitors and to gain insight into their structure-activity relationships (SAR). All compounds tested ...

In this study, Leydig cells were purified from 70 day-old Sprague Dawley male rats and incubated with 10 and 100 μg/mL of methanol extract of Basella alba (MEBa) for 4 hours followed by the evaluation of cell viability, steroid (testosterone and estradiol) production, and the level of aromatase mRNA. Results showed that MEBa did not affect Leydig cell viability. At the concentration of 10 μg/mL...