Aromatase Destabilizer: Novel Action of Exemestane, a Food and Drug Administration–Approved Aromatase Inhibitor
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چکیده
منابع مشابه
Aromatase destabilizer: novel action of exemestane, a food and drug administration-approved aromatase inhibitor.
Using Western blot as the major technique, we studied the effects of the three Food and Drug Administration (FDA)-approved aromatase inhibitors (AI) on aromatase protein stability in the aromatase-overexpressing breast cancer cell line MCF-7aro. We have found that exemestane treatment significantly reduces aromatase protein level. Exemestane induces aromatase degradation in a dose-responsive ma...
متن کاملIn vivo inhibition of aromatization by exemestane, a novel irreversible aromatase inhibitor, in postmenopausal breast cancer patients.
The effect of exemestane (6-methylenandrosta-1,4-diene-3,17-dione) 25 mg p.o. once daily on in vivo aromatization was studied in 10 postmenopausal women with advanced breast cancer. Aromatization was determined before treatment and after 6-8 weeks on therapy by administering a bolus injection of [3H]androstenedione (500 microCi) and [14C]estrone (5 microCi) followed by measurement of the isotop...
متن کاملEffects of the steroidal aromatase inhibitor exemestane and the nonsteroidal aromatase inhibitor letrozole on bone and lipid metabolism in ovariectomized rats.
PURPOSE Exemestane (EXE) and letrozole (LET) are third-generation aromatase inhibitors currently prescribed for postmenopausal hormone-dependent breast cancer. The impact on end organs of estrogen depletion in menopausal women is of significant clinical importance. We studied the effects of EXE, its principal metabolite, 17-hydroexemestane (17-H-EXE), and LET on bone and lipid metabolism in ova...
متن کاملAromatase over expression transgenic murine models for aromatase inhibitor studies.
In recent years the emerging importance of estrogen signaling in males in addition to its major role in the female reproductive system became highlighted. Aromatase is the key enzyme for synthesis of estrogens from androgens and is responsible for controlling the androgen/estrogen ratio. Inhibition of aromatase gene expression can be achieved in different ways and is important for the treatment...
متن کاملEfficacy of exemestane after nonsteroidal aromatase inhibitor use in metastatic breast cancer patients.
BACKGROUND Previous studies have suggested a lack of complete cross-resistance between steroidal (exemestane) and non-steroidal aromatase inhibitors (nSAI). METHODS Eighty-eight metastatic breast cancer (MBC) patients who received 25 mg of exemestane orally once a day at the National Cancer Center, Korea, between 2003 and 2009, were reviewed retrospectively. All patients had received nSAI for...
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ژورنال
عنوان ژورنال: Cancer Research
سال: 2006
ISSN: 0008-5472,1538-7445
DOI: 10.1158/0008-5472.can-06-2134