Mineralocorticoid Receptor Antagonists

The mineralocorticoid receptor (MR) is a member of the nuclear receptor family that mediates the biological action of aldosterone. This receptor has a critical role in the electrolyte homeostasis and blood pressure, and has been implicated in the development of cardiac fibrosis. MR antagonists might be useful in the treatment of severe cardiac failure and some forms of hypertension. However, the two antagonists currently approved for clinical use, spironolactone and eplerenone, display important side effects that limit their use.

The group is working on the search for new selective, non-steroidal small-molecule MR modulators, employing methods of computer-aided drug discovery. Our main strategy to identify MR ligands imply virtual screening studies and hit-to-lead optimization, assisted also by molecular modeling, to get potent and selective MR antagonists.