Epigenetic inhibitors attenuate pathological gene expression in cardiomyocytes

Epigenetic modulators have been proposed as promising new drug targets to treat adverse remodeling in heart failure. Here, we evaluated the potential of 4 epigenetic drugs, including the pan-BRD (bromodomain-containing protein) inhibitor bromosporine, the BET (bromodomain and extraterminal) inhibitor JQ1, more…

Approaches towards tissue-selective pharmacology of the mineralocorticoid receptor

Mineralocorticoid receptor antagonists (MRAs) are highly effective therapies for cardiovascular and renal disease. However, the widespread clinical use of currently available MRAs in cardiorenal medicine is hampered by an increased risk of hyperkalemia. The mineralocorticoid receptor (MR) is a nuclear more…

Endothelial cell mineralocorticoid receptors drive pulmonary hypertension and RV failure

Mineralocorticoid receptor (MR) antagonists are well established in the treatment of chronic left heart disease, however, there is an ever growing body of evidence suggesting potential benefits in other cardiovascular disease. Here, we evaluated the effects of MR antagonists on more…