Mineralocorticoid Receptor (E9W1M) Rabbit mAb #58883

Mineralocorticoid receptor (MR) is a steroid hormone receptor with structural and functional similarities to glucocorticoid receptor (GR). MR binds with high affinity to aldosterone and other mineralocorticoids as well as glucocorticoids (1-3). Upon ligand binding, MR undergoes conformational changes and enters the nucleus to bind to target mineralocorticoid response elements (MREs) (3-5). MR is also able to heterodimerize with GR and bind to hormone response elements on DNA in cells that express both receptors (6-8). Unlike the anti-inflammatory activity of GR, aldosterone and MR can promote cardiovascular inflammation (9,10). Since MR can utilize both aldosterone and glucocorticoids as ligands, selectivity of ligands is facilitated by tissue-specific expression of 11 beta-hydroxysteroid dehydrogenase (11 beta-OHSD). This enzyme converts cortisol to cortisone, a derivative with very little affinity to MR, thus providing a means for tissue-specific MR regulation (11,12). Deficiency of 11 beta-OHSD has shown to cause an excess of MR signaling resulting in hypertension (12,13). Antimineralocorticoid spirolactones have been used as synthetic steroids to induce a transcriptionally inactivated conformational change in MR to treat hypertension and sodium retention (14,15).