ArticleAmerican journal of cardiovascular disease2011
GRK2 and β-arrestins in cardiovascular disease: Something old, something new.
Article in American journal of cardiovascular disease, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed.
- The beta1-adrenergic receptor in the heart.Cell death discovery · 2025Review
- Uncovering conserved networks and global conformational changes in G protein-coupled receptor kinases.Computational and structural biotechnology journal · 2024Article
- Role of G-Proteins and GPCRs in Cardiovascular Pathologies.Bioengineering (Basel, Switzerland) · 2023Review
- GTPγS Assay for Measuring Agonist-Induced Desensitization of Two Human Polymorphic AlphaMethods in molecular biology (Clifton, N.J.) · 2022Article
- G Protein-Coupled Receptor Kinase 2 (GRK2) as a Potential Therapeutic Target in Cardiovascular and Metabolic Diseases.Frontiers in pharmacology · 2019Review
- Co-treatment with clonidine and a GRK2 inhibitor prevented rebound hypertension and endothelial dysfunction after withdrawal in diabetes.Hypertension research : official journal of the Japanese Society of Hypertension · 2018Article
- Adverse Effects on β-Adrenergic Receptor Coupling: Ischemic Postconditioning Failed to Preserve Long-Term Cardiac Function.Journal of the American Heart Association · 2017Article
- Multifaceted role of β-arrestins in inflammation and disease.Genes and immunity · 2015Review
- Effects of chronic treatment with the new ultra-long-acting β2 -adrenoceptor agonist indacaterol alone or in combination with the β1 -adrenoceptor blocker metoprolol on cardiac remodelling.British journal of pharmacology · 2015Article
- G-protein-coupled receptor kinase 2 and endothelial dysfunction: molecular insights and pathophysiological mechanisms.Journal of smooth muscle research = Nihon Heikatsukin Gakkai kikanshi · 2015Review
- Occipital Artery Function during the Development of 2-Kidney, 1-Clip Hypertension in Rats.International journal of vascular medicine · 2014Article
- Mitochondrial G protein coupled receptor kinase 2 regulates proinflammatory responses in macrophages.FEBS letters · 2013Article
- The role of G protein coupled receptor kinases in neurocardiovascular pathophysiology.Archives of medical science : AMS · 2012Article
Corrections and comments
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Authors and funding
1 author.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Heptahelical G protein-coupled receptors are the most diverse and therapeutically important family of receptors in the human genome, playing major roles in the physiology of various organs/tissues including the heart and blood vessels. Ligand binding activates heterotrimeric G proteins that transmit intracellular signals by regulating effector enzymes or ion channels. G protein signaling is terminated, in large part, by phosphorylation of the agonist-bound receptor by the family of G-protein coupled receptor kinases (GRKs) followed by βarrestin binding, which uncouples the phosphorylated receptor and G protein and subsequently targets the receptor for internalization. As the receptor-βarrestin complex enters the cell, βarrestins serve as ligand-regulated scaffolds that recruit a host of intracellular proteins and signal transducers, thus promoting their own wave of signal transduction independently of G-proteins. A large number of preclinical studies in small and large animals over the past several years have pinpointed specific pathophysiologic roles played by these two families of receptor-regulating proteins in various cardiovascular diseases, directly implicating them in disease pathology and suggesting them as potential therapeutic targets. The present review gives an account of what is currently known about the benefits of cardiac GRK2 inhibition for cardiovascular disease treatment, and also discusses the exciting new therapeutic possibilities emerging from uncovering the physiological roles of adrenal GRK2 and of βarrestin-mediated signaling in vivo in the cardiovascular system.
Indexed as
Identifiers
22254193PMC3253495What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.