Target intelligence / Profile preview

Aromatase (cytochrome P450 19A1) (CYP19A1)

Target
CYP19A1
Molecular classification
Enzyme, Cytochrome P450 monooxygenase
01

Overview

Aromatase is a cytochrome P450 monooxygenase encoded by the CYP19A1 gene. It catalyzes the conversion of C19 androgens (androstenedione, testosterone) into C18 estrogens (estrone, estradiol) via a three-step oxidation and aromatization mechanism. This enzyme is the only known vertebrate enzyme capable of aromatizing the steroid A-ring, making it essential in estrogen synthesis[1][4][8]. Expressed in multiple tissues—including gonads, adipose tissue, placenta, brain, and breast—aromatase regulates estrogen production critical for sexual development and reproductive function. Its overexpression is implicated in hormone-dependent breast cancer, providing a frontline therapeutic target for aromatase inhibitors, which reduce estrogen levels by inhibiting aromatase-mediated biosynthesis[2][5][7][8].

Other names
estrogen synthetaseestrogen synthaseCYP19CYP19A1
02

Mechanism of action

Competitive inhibition (non-steroidal inhibitors: reversible binding at the active site, e.g., anastrozole, letrozole)[3][6] Mechanism-based (suicide) inhibition (steroidal inhibitors form covalent bonds, irreversibly inactivating aromatase, e.g., exemestane)[3][6]

03

Biological functions

Estrogen biosynthesis (conversion of androgens to estrogens)Steroid metabolismRegulation of sexual development
04

Disease associations

Cancer (notably breast cancer, endometrial cancer)Reproductive dysfunction (including fertility-related disorders)Gynecomastia and estrogen imbalance syndromes
05

Safety considerations

Loss of bone mineral density (osteoporosis)Arthralgia (joint pain)Hot flashesIncreased risk of cardiovascular eventsHypercholesterolemiaMenopausal symptoms (particularly in postmenopausal women)[6]
06

Interacting drugs

Anastrozole

7 more in the full profile.

07

Biomarkers

CYP19A1 mRNA or protein levels (for predicting estrogen biosynthesis capacity and response to AIs)Estrogen levels (for monitoring efficacy in breast cancer therapy)Androgen/estrogen ratios

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