Beta-arrestin-biased ligands at the AT1R: a novel approach to the treatment of acute heart failure

The angiotensin II type 1 receptor (AT1R) is an important drug target for hypertension and chronic heart failure. This receptor is also important in the pathophysiology of acute heart failure, stimulating both adverse and beneficial hemodynamic and renal responses. This review will discuss advances in our understanding of the molecular mechanisms of AT1R function, and how these insights have enabled the discovery of β-arrestin-biased AT1R ligands, one of which is now in clinical trials for acute heart failure (AHF) treatment.