Aromatase (estrogen synthetase) is the enzyme complex responsible for the final step in estrogen synthesis--the conversion of androstenedione and testosterone to estrone and estradiol, respectively. Inhibitors of this enzyme have been shown to be clinically effective in the treatment of advanced breast cancer in postmenopausal women, in whom the major source of estrogen production derives from ...

INTRODUCTION Sex hormones, especially estrogens, have been implicated in articular cartilage metabolism and the pathogenesis of postmenopausal osteoarthritis. The conversion by aromatase (CYP19A1) of androstenedione into estrone (E1) and of testosterone into 17β-estradiol (E2) plays a key role in the endogenous synthesis of estrogens in tissue. METHODS We analyzed the expression of aromatase ...

7 alpha-(4'-Amino)phenylthio-1,4-androstadiene-3,17-dione (7 alpha-APTADD), a potent enzyme-activated irreversible inhibitor, was examined in two different human cell culture lines, MCF-7 human mammary carcinoma cells and JAr choriocarcinoma cells. Both the MCF-7 and JAr cell culture systems exhibit aromatase activity, and 7 alpha-APTADD was evaluated for its aromatase-inhibitory activity, for ...

BACKGROUND In order to reduce the risk of recurrence, adjuvant treatment with an aromatase inhibitor (AI) is recommended for postmenopausal women following surgery for hormone receptor-positive breast cancer. AIs are associated with improved disease-free survival compared with tamoxifen. The adverse events associated with AIs resemble those of menopause, such as bone density loss and musculoske...

The present study was undertaken to investigate the aromatization capability of pig corpora lutea at different stages of the luteal phase using the nonsteroidal aromatase inhibitor CGS 16949A. Luteal cells were collected during early (0-2 days after ovulation), mid- (7-10 days after ovulation) and late (13-16 days after ovulation) luteal phase. Cells were incubated either with or without 10(-7)...

PURPOSE To evaluate the efficacy of treatment with the aromatase inhibitor letrozole in breast cancer patients segregated with respect to DNA polymorphisms of the aromatase gene CYP19. PATIENTS AND METHODS Postmenopausal patients (n = 67) with hormone receptor-positive metastatic breast cancer were treated with the aromatase inhibitor letrozole. PCR allelic discrimination was used to examine ...

Purpose: Lung adenocarcinomas amongnever-smokers aremore common in females than inmales. This implies that gender-dependent hormones promote smoking unrelated lung adenocarcinoma. We therefore investigated mRNA expression of aromatase, an intrinsic estrogen synthetase, in lung adenocarcinoma and assessed its correlation to clinicopathologic factors, including EGFRmutations and postsurgical prog...

For many oncologists, neoadjuvant treatment for breast cancer is synonymous with preoperative cytotoxic chemotherapy, regardless of tumor characteristics. Preoperative therapy with an endocrine agent is generally considered suitable only for the frail elderly or the medically unfit. However, favorable information regarding third-generation aromatase inhibitors in the treatment of all stages of ...

PURPOSE Circulating and cellular proangiogenic and antiangiogenic proteins such as vascular endothelial growth factor (VEGF) and endostatin contribute to the local angiogenic balance. We explored the effects of tamoxifen and aromatase inhibitors on concentrations of VEGF and endostatin in plasma, serum, and platelet releasate (induced by platelet activation). EXPERIMENTAL DESIGN VEGF and endo...