Mineralocorticoid ReceptorEndocrine disruption: Estimation of the binding affinity of small molecules towards the Mineralocorticoid receptor.
The mineralocorticoid receptor plays an important role in the regulation of renal sodium reabsorption and blood pressure control. Several recent studies provided evidence for a key role of the activation of MR in macrophage during inflammatory processes. However, the role of the mineralocorticoid receptor in macrophage remains largely unknown. Clinical trials revealed an approximately 30% reduced rate of mortality in patients with heart failure upon treatment with the MR antagonist spironolactone or eplerenone. In these patients, aldosterone concentrations are normal or even lower than in control individuals. In some studies, it is hypothesized that the mineralocorticoid receptor might be activated by the glucocorticoid cortisol, while other studies suggest a ligand-independent receptor activation by translational modification.
Mineralocorticoid receptor with bound Erythrosine.
Comparison of experimental and predicted Ki values for the mineralocorticoid receptor
(training set = black, test set = red).