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Aromatase (CYP19A1) is a membrane-bound enzyme of the cytochrome P450 superfamily that catalyzes the final and rate-limiting step in the production of estrogens: the aromatization of androgens (such as testosterone and androstenedione) to estrogens (estradiol and estrone)[1][3]. Aromatase is expressed primarily in the ovaries, and also in adipose tissue, brain, bone, and other sites outside the gonads[7]. Inhibition of aromatase is a principal therapeutic strategy for treating estrogen receptor–positive breast cancer and certain other estrogen-dependent diseases. Aromatase is distinct from estrogen receptors (ERα, ERβ), which mediate the effects of estrogens but are not responsible for their synthesis[1][2][4][6].
Competitive inhibition of aromatase, reducing the synthesis of estrogens from androgenic precursors Irreversible inactivation (for steroidal inhibitors like exemestane) Reduction in estrogen-mediated signaling and cellular proliferation in estrogen-responsive tissues
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