Target intelligence / Profile preview

Cytochrome P450 aromatase (CYP19A1)

Target
CYP19A1
Molecular classification
Enzyme, Cytochrome P450 family, Monooxygenase
01

Overview

Cytochrome P450 aromatase (CYP19A1) is a monooxygenase enzyme of the cytochrome P450 superfamily and the sole enzyme responsible for catalyzing the aromatization of androgens (such as androstenedione and testosterone) into estrogens (estrone and estradiol) during the final step of estrogen biosynthesis. It is predominantly localized in the endoplasmic reticulum of estrogen-producing tissues, including the gonads, brain, adipose tissue, placenta, bone, and various pathological sites (e.g., hormone-dependent tumors). Aromatase is essential for normal female sexual development, fertility, and bone health, and its dysregulation or overexpression is implicated in several estrogen-dependent diseases, especially hormone receptor–positive cancers. Aromatase inhibitors, which block its enzymatic function, are established therapeutics in postmenopausal breast cancer and are being studied or used in other estrogen-mediated disorders[1][3][4][7].

Other names
AromataseEstrogen synthetaseEstrogen synthaseCYP19Cytochrome P450 19A1
02

Mechanism of action

Inhibition of aromatase enzyme activity, preventing conversion of androgens to estrogens and decreasing estrogen biosynthesis

03

Biological functions

Estrogen biosynthesisSteroidogenesisSexual developmentRegulation of reproductive physiology
04

Disease associations

Cancer (notably breast and endometrial cancer)EndometriosisUterine fibroidsDisorders of sexual developmentOther estrogen-dependent conditions
05

Safety considerations

Estrogen deficiency (hot flashes, osteoporosis, cardiovascular risk, arthralgia, mood changes)Loss of fertilityPotential adverse effects on bone density and lipid profiles
06

Interacting drugs

Letrozole

5 more in the full profile.

07

Biomarkers

CYP19A1 mRNA or protein expression in tumor or adipose tissueCirculating estrogen levels (estradiol, estrone)

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