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Aromatase, Aromatase Inhibitors, and Breast Cancer
American Journal of Therapeutics, 2001Estrogens are involved in numerous physiologic processes and have crucial roles in particular disease states, such as mammary carcinomas. Estradiol, the most potent endogenous estrogen, is biosynthesized from androgens by the cytochrome P-450 enzyme complex called aromatase.
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Aromatase Overexpression: Is Aromatase an Oncogene
2001To directly test the role of aromatase overexpression in tumorigenesis, we have developed a transgenic mouse model and demonstrated for the first time that increased tissue estrogens due to the overexpression of aromatase in mammary glands leads to the induction of various preneoplastic and neoplastic changes that are similar to early breast cancer ...
Rajeshwar Rao Tekmal +2 more
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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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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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The Journal of Steroid Biochemistry and Molecular Biology, 2003
Aromatase gene expression and activity have been studied in human skeletal muscle. Using two separate rounds of RT-nested PCR, transcripts from the coding region of aromatase mRNA were detected in 32 of 34 samples. In terms of the non-coding exon I, PCR product for I.4 was detected in 13 cases (38%), I.3 in 10 cases (29%), P.II in 6 cases (18%) and I.1
A A, Larionov +5 more
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Aromatase gene expression and activity have been studied in human skeletal muscle. Using two separate rounds of RT-nested PCR, transcripts from the coding region of aromatase mRNA were detected in 32 of 34 samples. In terms of the non-coding exon I, PCR product for I.4 was detected in 13 cases (38%), I.3 in 10 cases (29%), P.II in 6 cases (18%) and I.1
A A, Larionov +5 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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