Aromatase and Its Inhibitors
Estrogens are involved in numerous physiological processes including the development and maintenance of the female sexual organs, the reproductive cycle, reproduction, and various other neuroendocrine functions. These hormones have crucial roles in certain disease states, particularly in mammary and endometrial hyperplasias and breast cancers.
Estrogens are biosynthesized from androgens by the cytochrome P450 enzyme complex called “aromatase” first discovered in 1955.
The aromatase enzyme complex is bound in the endoplasmic reticulum of the cell and is comprised of two major proteins. One protein is cytochrome P450arom, a hemoprotein that converts C19 steroids (androgens) into C18 steroids (estrogens) containing a phenolic A ring. The second protein is NADPH-cytochrome P450 reductase, which transfers reducing equivalents to cytochrome P450arom. Three moles of NADPH and three moles of oxygen are...
KeywordsPostmenopausal Woman Aromatase Inhibitor Advanced Breast Cancer Estrogen Synthesis Estrone Sulfate
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