Target intelligence / Profile preview

Aromatase (Cytochrome P450, family 19, subfamily A, polypeptide 1) (CYP19A1)

Target
CYP19A1
Molecular classification
Enzyme, Cytochrome P450 superfamily, Monooxygenase, Oxidoreductase
01

Overview

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].

Other names
Estrogen synthetaseCYP19Estrogen synthaseCytochrome P450 19A1
02

Mechanism of action

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

03

Biological functions

Estrogen biosynthesis (conversion of androgens to estrogens)Steroid hormone metabolismRegulation of sexual development and reproductionModulation of cell proliferation and apoptosis, especially in estrogen-sensitive tissues
04

Disease associations

Cancer (notably hormone-dependent breast cancer, endometrial cancer)EndometriosisGynecomastiaOsteoporosis (postmenopausal estrogen deficiency)Disorders of sexual development
05

Safety considerations

Menopausal symptoms (hot flashes, vaginal dryness)Decreased bone mineral density/osteoporosisArthralgias and myalgiasIncreased cardiovascular risk (possibly with long-term use)Negative effects on lipid metabolism
06

Interacting drugs

Anastrozole

4 more in the full profile.

07

Biomarkers

CYP19A1 (aromatase) expression levels (tumor tissue, plasma)Estradiol/estrogen concentration (plasma, tissue)Estrogen receptor (ER) expression (ERα, ERβ)Response to aromatase inhibitor treatment in hormone receptor–positive cancers

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