Vol 61, No 1 (2010)
Review paper
Submitted: 2013-02-15
Published online: 2010-03-04
Aromatase research and its clinical significance
Izabella Czajka-Oraniec, Evan R. Simpson
Endokrynol Pol 2010;61(1):126-134.
Vol 61, No 1 (2010)
Review Article
Submitted: 2013-02-15
Published online: 2010-03-04
Abstract
Aromatase is a member of the cytochrome P450 superfamily that catalyzes the conversion of androgens (C19), namely testosterone and
androstenedione, into oestrogens (C18), oestradiol, and oestrone, respectively. The enzyme is active in various tissues in both females and
males, thus oestrogens are produced not only in gonads but also in extra-gonadal localizations such as brain, adipose tissue, breast, skin,
and bone. Aromatase gene CYP19A1 located on chromosome 15 comprises nine coding exons and a number of alternative non-coding first
exons that regulate tissue-specific expression. Studies on local regulation of aromatase expression and activity are important for understanding
processes such as growth of oestrogen-dependent breast cancer. Rare clinical conditions of aromatase deficiency and excess have
revealed some new and unexpected oestrogen functions in metabolism and bone health in both women and men. They were further
studied using transgenic animal models such as aromatase knockout mice (ArKO) or (AROM+) mice overexpressing human aromatase.
Research on aromatase was important for its practical outcome as it contributed to the development of aromatase inhibitors (AIs), an
effective and safe group of drugs for the first-line endocrine therapy of breast cancer. Further studies are needed to establish AIs application
in other oestrogen-dependent conditions, to overcome the resistance in breast cancer patients, and to develop tissue-specific selective
inhibitors. (Pol J Endocrinol 2010; 61 (1): 126–134)
Abstract
Aromatase is a member of the cytochrome P450 superfamily that catalyzes the conversion of androgens (C19), namely testosterone and
androstenedione, into oestrogens (C18), oestradiol, and oestrone, respectively. The enzyme is active in various tissues in both females and
males, thus oestrogens are produced not only in gonads but also in extra-gonadal localizations such as brain, adipose tissue, breast, skin,
and bone. Aromatase gene CYP19A1 located on chromosome 15 comprises nine coding exons and a number of alternative non-coding first
exons that regulate tissue-specific expression. Studies on local regulation of aromatase expression and activity are important for understanding
processes such as growth of oestrogen-dependent breast cancer. Rare clinical conditions of aromatase deficiency and excess have
revealed some new and unexpected oestrogen functions in metabolism and bone health in both women and men. They were further
studied using transgenic animal models such as aromatase knockout mice (ArKO) or (AROM+) mice overexpressing human aromatase.
Research on aromatase was important for its practical outcome as it contributed to the development of aromatase inhibitors (AIs), an
effective and safe group of drugs for the first-line endocrine therapy of breast cancer. Further studies are needed to establish AIs application
in other oestrogen-dependent conditions, to overcome the resistance in breast cancer patients, and to develop tissue-specific selective
inhibitors. (Pol J Endocrinol 2010; 61 (1): 126–134)
Keywords
aromatase; oestrogens; androgens; aromatase inhibitors; breast cancer
Title
Aromatase research and its clinical significance
Journal
Endokrynologia Polska
Issue
Vol 61, No 1 (2010)
Article type
Review paper
Pages
126-134
Published online
2010-03-04
Page views
1313
Article views/downloads
3441
Bibliographic record
Endokrynol Pol 2010;61(1):126-134.
Keywords
aromatase
oestrogens
androgens
aromatase inhibitors
breast cancer
Authors
Izabella Czajka-Oraniec
Evan R. Simpson
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