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Aromatase Inhibitors as Chemopreventives of Breast Cancer

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Cancer Chemoprevention

Part of the book series: Cancer Drug Discovery and Development ((CDD&D))

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Abstract

Aromatase is a cytochrome P450 enzyme present in the endoplasmic reticulum (ER) which is responsible for the synthesis of steroidal estrogens. It appears that a single aromatase gene codes for the enzyme in all tissues, but, as discussed here, the control of this gene is tissue-specific according to the usage of a number of different promoters (1). Aromatase catalyzes the conversion of androstenedione (the preferred substrate) and testosterone to estrone, then to estradiol. The conversion of estrone to estradiol the most potent estrogen is reversible, and is catalyzed by the 17(β hydroxysteroiddehydrogenase enzyme system (Fig. 1).

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Dowsett, M., Garber, J.E. (2004). Aromatase Inhibitors as Chemopreventives of Breast Cancer. In: Kelloff, G.J., Hawk, E.T., Sigman, C.C. (eds) Cancer Chemoprevention. Cancer Drug Discovery and Development. Humana Press, Totowa, NJ. https://doi.org/10.1007/978-1-59259-767-3_15

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