Target intelligence / Profile preview

Cytochrome P450 11B2, mitochondrial (CYP11B2)

Target
CYP11B2
Molecular classification
Enzyme, Cytochrome P450 monooxygenase, Mitochondrial protein
01

Overview

Cytochrome P450 11B2, mitochondrial (CYP11B2), commonly known as **aldosterone synthase**, is a mitochondrial cytochrome P450 enzyme primarily expressed in the zona glomerulosa of the adrenal cortex. It catalyzes the final steps in the biosynthesis of the mineralocorticoid hormone aldosterone, which is crucial for maintaining salt and water homeostasis and thus regulates blood pressure and electrolyte balance. CYP11B2 is the only enzyme in humans capable of converting 11-deoxycorticosterone sequentially to corticosterone, 18-hydroxycorticosterone, and ultimately to aldosterone. Dysregulation of CYP11B2, due to genetic mutations or abnormal expression, is linked to diseases such as primary aldosteronism, familial hyperaldosteronism, and corticosterone methyloxidase deficiency. Variants in the gene have also been associated with increased risk of cardiovascular diseases including hypertension, heart failure, and stroke. Aldosterone synthase is a therapeutic target for the treatment of hypertension and related cardiovascular diseases, with both direct enzyme inhibitors and downstream antagonists (such as spironolactone and eplerenone) used clinically or in development.

Other names
Aldosterone synthaseAldosterone-synthesizing enzymeCorticosterone 18-monooxygenaseSteroid 18-hydroxylaseSteroid 11-beta-hydroxylaseCytochrome P-450C18Cytochrome P-450AldoP450C18P450aldoCPN2ALDOSCYPXIB2C11B2_HUMANMitochondrial cytochrome P450, family 11, subfamily B, polypeptide 2
02

Mechanism of action

Inhibition of aldosterone synthesis; antagonism of aldosterone receptor effects (by lowering aldosterone levels via enzyme blockade); direct enzyme inhibition (as in experimental CYP11B2 inhibitors).

03

Biological functions

Aldosterone biosynthesisSteroidogenesisRegulation of electrolyte balanceBlood pressure regulationSalt and water homeostasis
04

Disease associations

Cardiovascular diseaseHypertensionFamilial hyperaldosteronism/Primary aldosteronismCorticosterone methyloxidase deficiency (aldosterone synthase deficiency)Stroke (associated polymorphisms)Heart failure (atrial fibrillation risk)
05

Safety considerations

Potential for adrenal insufficiency or hypoaldosteronism with excessive or off-target inhibitionElectrolyte disturbances (hyponatremia, hyperkalemia)Blood pressure dysregulation (risk of hypotension)
06

Interacting drugs

Spironolactone (targeted indirectly as aldosterone antagonist)

4 more in the full profile.

07

Biomarkers

Aldosterone levels (for diagnosis/monitoring in hyperaldosteronism)Plasma renin activity (used in workflows for primary aldosteronism diagnosis)Immunohistochemical detection of CYP11B2 (to localize aldosterone-producing cell clusters)18-oxocortisol and 18-hydroxycortisol (biomaterial markers in primary aldosteronism)

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