Aromatase (also known as CYP19) is a member of the general class of cytochrome P450 enzymes. It catalyzes the conversion of androgens to estrogens, which is a crucial step in the biosynthesis of estrogens in the human body.
Aromatase enzyme is expressed in ovarian granulosa cells, placental syncytiotrophoblast, adipose tissue, brain, and skin fibroblasts. The primary sources of aromatase are ovarian granulosa cells in premenopausal women and adipose cells in postmenopausal women. Aromatase inhibitors suppress oestrogen synthesis in the ovaries and in peripheral tissues, starting from the next day after dosing. They work by inhibiting the action of aromatase, which converts androgens into oestrogens (testosterone into estradiol and androstenedione into oestrone). There are three generations of aromatase inhibitors (AIs). Aminoglutethimide is a first-generation aromatase inhibitor. The second-generation inhibitors include Fadrozole and Formestane. Anastrozole, Letrozole, and Exemestane are third-generation inhibitors.
Aromatase is encoded by the cyp19a1 gene, belongs to a particular reticulum-bound cytochrome P450 superfamily and forms an electron-transfer complex with its partner, NADPH-cytochrome P450 reductase (CPR).
||Letrozole(CGS-20267) is an oral non-steroidal aromatase inhibitor that has been introduced for the adjuvant.
||Fadrozole is a potent, selective and nonsteroidal inhibitor of aromatase with an IC50 of 6.4 nM.
||A potent aromatase inhibitor for the treatment of hypogonadism..