The G protein coupled receptor kinase 2 plays an essential role in beta-adrenergic receptor-induced insulin resistance [PDF]
Insulin (Ins) resistance (IRES) associates to increased cardiovascular risk as observed in metabolic syndrome. Chronic stimulation of beta-adrenergic receptors (betaAR) due to exaggerated sympathetic nervous system activity is involved in the pathogenesis of IRES. The cellular levels of G protein coupled receptor kinase 2 (GRK2) increase during chronic
E. Cipolletta +7 more
openaire +4 more sources
Systemic aging fuels heart failure: Molecular mechanisms and therapeutic avenues
Abstract Systemic aging influences various physiological processes and contributes to structural and functional decline in cardiac tissue. These alterations include an increased incidence of left ventricular hypertrophy, a decline in left ventricular diastolic function, left atrial dilation, atrial fibrillation, myocardial fibrosis and cardiac ...
Zhuyubing Fang +7 more
wiley +1 more source
Cyclic AMP signalling in pancreatic islets [PDF]
Cyclic 3'5'AMP (cAMP) is an important physiological amplifier of glucose-induced insulin secretion by the pancreatic islet β-cell, where it is formed by the activity of adenylyl cyclases, which are stimulated by glucose, through elevation in ...
Furman, Brian +2 more
core +1 more source
Sequeira et al. reveal how the glucagon‐like peptide‐1 receptor agonist (GLP‐1‐RA) semaglutide restores cardiomyocyte function in rats subjected to a high‐fat/high‐fructose diet (HFD). Employing fluorescence‐ and patch‐clamp technology in isolated cardiac myocytes, they demonstrate that semaglutide reverses HFD‐induced activation of L‐type calcium ...
Vasco Sequeira +12 more
wiley +1 more source
Phosphorylation and Activation of β-Adrenergic Receptor Kinase by Protein Kinase C [PDF]
The aim of this study was to test the possible modification of beta-adrenergic receptor kinase (beta ARK) activity by second messengers and/or their downstream components. Using human mononuclear leukocytes (MNL), we found that calcium ionophores could elevate beta ARK activity by about 80% in a protein kinase C (PKC)-dependent manner.
Chuang TT +2 more
openaire +4 more sources
Cilostazol in patients with heart failure and preserved ejection fraction—The CLIP‐HFpEF trial
• Cilostazol is an oral PDE‐3 inhibitor that may have advantageous effects in heart failure with preserved ejection fraction (HFpEF). • Cilostazol significantly improved short‐term heart failure‐related health status scores (KCCQ‐12) and NT‐proBNP levels when compared to placebo.
Norman Aiad +9 more
wiley +1 more source
β-adrenergic receptors and G protein-coupled receptor kinase-2 in Alzheimer's disease: a new paradigm for prognosis and therapy? [PDF]
Alzheimer's disease (AD) is a devastating form of dementia that imposes a severe burden on health systems and society. Although several aspects of AD pathogenesis have been elucidated over the last few decades, many questions still need to be addressed ...
Cannavo A +11 more
core +1 more source
Status epilepticus: Updates on mechanisms and treatments
Abstract Status epilepticus (SE) consists of prolonged, self‐sustaining seizures and is a common neurological emergency that causes respiratory compromise and neuronal injury. Without prompt treatment, the seizures can become resistant to benzodiazepines, leading to the progressive evolution of established, refractory, and super‐refractory SE.
Suchitra Joshi, Jaideep Kapur
wiley +1 more source
Mapping the druggable allosteric space of G-protein coupled receptors: a fragment-based molecular dynamics approach. [PDF]
To address the problem of specificity in G-protein coupled receptor (GPCR) drug discovery, there has been tremendous recent interest in allosteric drugs that bind at sites topographically distinct from the orthosteric site. Unfortunately, structure-based
Ivetac, Anthony, McCammon, J Andrew
core +2 more sources
Desensitization of the beta-adrenergic receptor, a receptor which is coupled to the stimulation of adenylate cyclase, may be regulated via phosphorylation by a unique protein kinase. This recently discovered enzyme, known as the beta-adrenergic receptor kinase, only phosphorylates the agonist-occupied form of the beta-adrenergic receptor.
BENOVIC J. L +7 more
openaire +2 more sources

