Mineralocorticoid receptor
FunctionMineralocorticoid receptor (MR) in epithelial cells is activated by the mineralocorticoid hormone aldosterone promoting renal sodium retention and potassium excretion. It is nuclear receptor. In non epithelial cells MR is activated by cortisol[1]. MR is exposed to many steroids including cortisol, cortisone and progesterone, however, aldosterone and deoxycorticosterone are its physiological ligands. See also Mineralocorticoids; Steroid Hormones and their receptors and Intracellular receptors DiseaseMR mutations are the principal cause of renal pseudohypoaldosteronism[2]. MR mutation S810L causes early-onset hypertension[3]. RelevanceInhibition of cardia MR prevents doxorubicin-induced cardiotoxicity[4]. MR is an important proadipogenic transcription factor that may mediate aldosterone and glucocorticoid effects on adipose tissue development and hence on obesity and development of metabolic syndrome[5]. Structural highlightsThe MR ligand aldosterone binds in a fully enclosed pocket, contacting residues with six α-helices and a β-turn (Alpha Helices, Beta Strands , Loops , Turns). It forms hydrogen bonds with 4 MR residues[6]. Whole binding site. Water molecules are shown as red spheres.
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3D Structures of mineralocorticoid receptor
Updated on 19-January-2023
- Mineralocorticoid receptor DNA-binding site residues 593-671
- nuclear receptor – hMR DBD + DNA - human
- nuclear receptor – hMR DBD + DNA - human
- Mineralocorticoid receptor DNA-binding site residues 712-984
- Mineralocorticoids – hMR LBD (mutant) + aldosterone
- Steroid Hormones and their receptors, Intracellular receptors , 1ya3– hMR LBD (mutant) + progesterone
- 2aa7, 2abi, 1y9r – hMR LBD (mutant) + deoxycorticosterone
- 2aax – hMR LBD (mutant) + cortisone
- 2ab2, 3vhu, 2oax – hMR LBD (mutant) + spironolactone
- 3wff, 3wfg, 4pf3, 3vhv, 5hcv – hMR LBD (mutant) + antagonist
- 6l88 – hMR LBD (mutant) + esaxerenone
- 5mwy, 6gev – hMR LBD + NCOA1 peptide
- 2a3i, 5mwp – hMR LBD (mutant) + NCOA1 peptide
- 5l7e, 5l7g, 5l7h, 4uda, 4udb, 6gg8, 6ggg – hMR LBD + NCOA1 peptide + antagonist
- Mineralocorticoids – hMR LBD (mutant) + aldosterone