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Pharmacogenetics of Aromatase Inhibitors
Pharmacogenomics, 2012Aromatase inhibitors (AIs) are an important class of endocrine drugs used in the treatment of early and advanced breast cancer in postmenopausal women. A number of studies have taken candidate approaches to assess the role of variants in genes encoding enzymes important in AI metabolism, notably CYP19A1 (aromatase), in AI response.
Hadfield, Kristen D. +1 more
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Regulation of aromatase in cancer
Molecular and Cellular Biochemistry, 2021The regulation of aromatase, an enzyme involved in the biosynthesis of estrogen in normal and cancer cells, has been associated with growth factor signaling and immune response modulation. The tissue-specific regulatory roles of these factors are of particular importance as local aromatase expression is strongly linked to cancer development/progression
Deborah Molehin +3 more
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Binding characteristics of aromatase inhibitors and phytoestrogens to human aromatase
The Journal of Steroid Biochemistry and Molecular Biology, 1997We have evaluated the binding characteristics of three steroidal inhibitors [4-hydroxyandrostenedione (4-OHA), 7alpha-(4'-amino)phenylthio-1,4-androstadiene-3,17-dione (7alpha-APTADD), and bridge (2,19-methyleneoxy) androstene-3,17-dione (MDL 101,003)], four nonsteroidal inhibitors [aminoglutethimide (AG), CGS 20267, ICI D1033, and vorozole (R83842 ...
S, Chen, Y C, Kao, C A, Laughton
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The intratumoral aromatase model: studies with aromatase inhibitors and antiestrogens
The Journal of Steroid Biochemistry and Molecular Biology, 2003Aromatase inhibitors have now been approved as first-line treatment options for hormone-dependent advanced breast cancer. When compared to tamoxifen, these aromatase inhibitors provide significant survival and tolerability advantages. However, the optimal use of an aromatase inhibitor and tamoxifen remains to be established.
Angela H, Brodie +2 more
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A photoaffinity inhibitor of aromatase
Steroids, 1982Several 7 alpha-substituted 4-androstene-3,17-diones are potent inhibitors of the biosynthesis of estrogens, with the most effective being 7 alpha-(4'-amino)phenylthio-4-androstene-3,17-dione. An azide derivative of this 7 alpha-thioether compound has been prepared as a potential photoaffinity inhibitor.
R W, Brueggemeier +2 more
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Journal de la Societe de biologie, 2002
The cytochrome P450 aromatase (P450arom) is the terminal enzyme involved in the irreversible transformation of androgens into estrogens. The P450arom plays a role in development, reproduction, sexual differentiation and behaviour, but also in bone and lipid metabolisms, brain functions and diseases such as breast and testicular tumors.
Carreau, Serge +3 more
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The cytochrome P450 aromatase (P450arom) is the terminal enzyme involved in the irreversible transformation of androgens into estrogens. The P450arom plays a role in development, reproduction, sexual differentiation and behaviour, but also in bone and lipid metabolisms, brain functions and diseases such as breast and testicular tumors.
Carreau, Serge +3 more
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Arthralgia and aromatase inhibitors
Joint Bone Spine, 2014Joint Bone Spine - In Press.Proof corrected by the author Available online since mercredi 14 aout ...
Daniel, Wendling +4 more
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The Journal of Steroid Biochemistry and Molecular Biology, 1999
Inhibitors of aromatase (estrogen synthetase) have been developed as treatment for postmenopausal breast cancer. Both steroidal substrate analogs, type I inhibitors, which inactivate the enzyme and non-steroidal competitive reversible, type II inhibitors, are now available.
A, Brodie, Q, Lu, B, Long
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Inhibitors of aromatase (estrogen synthetase) have been developed as treatment for postmenopausal breast cancer. Both steroidal substrate analogs, type I inhibitors, which inactivate the enzyme and non-steroidal competitive reversible, type II inhibitors, are now available.
A, Brodie, Q, Lu, B, Long
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Toxicity of Aromatase Inhibitors
Seminars in Oncology, 2006Adjuvant hormonal therapy in hormone receptor-positive breast cancer is used for the prevention of disease recurrence and prolongation of survival. Aromatase inhibitors are increasingly being used for this purpose. Numerous studies now reveal their benefits over tamoxifen while demonstrating a markedly different toxicity profile.
Pandya, Naushira, Morris, G J
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Aromatase inhibition by flavonoids
The Journal of Steroid Biochemistry and Molecular Biology, 1990Several synthetic flavones were found to inhibit the aromatization of androstenedione to estrone catalyzed by human placental microsomes. Twenty-one compounds were tested and the IC50 of the most active were: flavone, 10 microM; 7-hydroxyflavone, 0.5 microM; 7,4'-dihydroxyflavone, 2.0 microM; flavanone, 8.0 microM; and 4'-hydroxyflavanone, 10 microM ...
A R, Ibrahim, Y J, Abul-Hajj
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