Key result
AT1 receptor β-arrestin biased agonists show therapeutic promise in CVD, but clinical efficacy remains unproven.
Why the study?
Understanding the role of beta-arrestins in cardiovascular conditions is critical to identify new therapeutic targets for the treatment of cardiovascular disease.
This review summarizes the beneficial and maladaptive physiological outcomes of angiotensin-II type 1 receptor-dependent β-arrestin activation in cardiovascular diseases.
May inform biased AT1 agonist development for cardiovascular disease; leaves open clinical efficacy pending randomized trials.
β-arrestins are a family of intracellular signaling proteins that play a key role in regulating the activity of G protein-coupled receptors. The angiotensin-II type 1 receptor is an important G protein-coupled receptor involved in the regulation of cardiovascular function and has been implicated in the progression of cardiovascular diseases. In addition to canonical G protein signaling, G protein-coupled receptors including the angiotensin-II type 1 receptor can signal via β-arrestin. Dysregulation of β-arrestin signaling has been linked to several cardiovascular diseases including hypertension, atherosclerosis, and heart failure. Understanding the role of β-arrestins in these conditions is critical to provide new therapeutic targets for the treatment of cardiovascular disease. In this review, we will discuss the beneficial and maladaptive physiological outcomes of angiotensin-II type 1 receptor-dependent β-arrestin activation in different cardiovascular diseases.
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Mathieu et al. (2023) conducted a review in Cardiovascular disease. AT1 receptor beta-arrestin biased agonists was evaluated. Activation of AT1 receptor-dependent β-arrestin signaling using biased agonists offers a novel therapeutic approach for cardiovascular diseases, though clinical efficacy remains to be fully established.
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