Structure–function relationships in the mineralocorticoid receptor

Structure-function relationships in the mineralocorticoid receptor.

The signature action of aldosterone in the regulation of electrolyte and fluid balance is well established. However, the role of aldosterone as an important contributor to morbidity and mortality in heart failure has gained a heightened interest in recent years, but the mechanisms of this action are not well understood. Aldosterone is the principal physiological ligand for the mineralocorticoid...

1 Structure - function relationships in the Mineralocorticoid Receptor

The Promiscuous Mineralocorticoid Receptor.

The article by Briet et al in this issue, “Aldosterone-induced vascular remodeling and endothelial dysfunction require functional angiotensin type 1a receptors,” represents a prodigious amount of work by the authors: it is not surprising that the first 3 are credited as having equally contributed. The authors build on previous in vitro studies, generously cited, on the interactions between mine...

Antagonism in the human mineralocorticoid receptor.

Key residues of the human mineralocorticoid receptor (hMR) involved in the recognition of agonist and antagonist ligands were identified by alanine-scanning mutagenesis based on a homology model of the hMR ligand-binding domain. They were tested for their transactivation capacity and ability to bind agonists (aldosterone, cortisol) and antagonists (progesterone, RU26752). The three-dimensional ...

30 YEARS OF THE MINERALOCORTICOID RECEPTOR: Evolution of the mineralocorticoid receptor: sequence, structure and function.

The mineralocorticoid receptor (MR) is descended from a corticoid receptor (CR), which has descendants in lamprey and hagfish, cyclostomes (jawless fish), a taxon that evolved at the base of the vertebrate line. A distinct MR and GR first appear in cartilaginous fishes (Chondrichthyes), such as sharks, skates, rays and chimeras. Skate MR has a strong response to corticosteroids that are mineral...