Cytochrome P450 11B2 (Aldosterone synthase) (CYP11B2)

Aldosterone synthase, specifically the rat ortholog of Cytochrome P450 11B2, is a mitochondrial enzyme primarily expressed in the zona glomerulosa of the adrenal cortex [UniProt: P15393]. It catalyzes the final three steps of aldosterone biosynthesis: the 11-beta-hydroxylation of 11-deoxycorticosterone to corticosterone, followed by 18-hydroxylation and 18-oxidation to produce aldosterone [PubMed: 1988126]. In rats, this enzyme is a critical target for preclinical research into mineralocorticoid-driven pathologies such as hypertension and cardiac fibrosis [PubMed: 21123461]. Excessive aldosterone production contributes significantly to cardiovascular and renal damage, making the inhibition of this enzyme a key therapeutic strategy. Aldosterone synthase inhibitors (ASIs) are designed to selectively block CYP11B2 while sparing the closely related CYP11B1 enzyme, which is responsible for glucocorticoid synthesis [PubMed: 36322151]. Rat models are frequently utilized to assess the potency and selectivity of these inhibitors before clinical progression in humans.

Other names

Aldosterone synthaseSteroid 18-hydroxylaseP450C18Cytochrome P450 family 11 subfamily B member 2Cyp11b2Corticosterone 18-monooxygenase

Inhibition of the enzymatic conversion of 11-deoxycorticosterone to aldosterone by blocking the 11-beta-hydroxylase, 18-hydroxylase, and 18-oxidase activities of the CYP11B2 protein.