Gosset Aldosterone Receptor Overview
The aldosterone receptor (MR), also known as NR3C2, is a nuclear hormone receptor that functions as a ligand-activated transcription factor. It plays a key role in regulating sodium reabsorption, potassium excretion, and blood pressure, primarily in the kidney, colon, heart, and central nervous system. Aldosterone is the primary physiological agonist, although cortisol and corticosterone can also bind with high affinity. Selectivity for aldosterone is achieved in some tissues by the enzyme 11β-HSD2. Antagonists like spironolactone and eplerenone are used therapeutically for conditions such as heart failure and hypertension. Mutations or overactivation of the MR can lead to hypertension and hypokalemia.
Mechanism of Action
Ligand binds to cytoplasmic MR, complex translocates into nucleus, binds hormone response elements on DNA, and modulates transcription of target genes.
Biological Functions
Disease Associations
Safety Considerations
- Overactivation or mutation can cause hypertension.
- Excessive sodium retention
- Hypokalemia