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
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
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
Gαq and its \u3ci\u3eAkt\u3c/i\u3eions [PDF]
No abstract ...
Eckhart, Andrea D. +2 more
core +1 more source
Considering the role of Murine double minute 2 in the cardiovascular system [PDF]
The E3 ubiquitin ligase Murine double minute 2 (MDM2) is the main negative regulator of the tumor protein p53 (TP53). Extensive studies over more than two decades have confirmed MDM2 oncogenic role through mechanisms both TP53-dependent and TP53 ...
Lam, Brian, Roudier, Emile
core +1 more source
Phosphorylation of Src by phosphoinositide 3-kinase regulates beta-adrenergic receptor-mediated EGFR transactivation [PDF]
β2-Adrenergic receptors (β2AR) transactivate epidermal growth factor receptors (EGFR) through formation of a β2AR-EGFR complex that requires activation of Src to mediate signaling. Here, we show that both lipid and protein kinase activities of the bifunctional phosphoinositide 3-kinase (PI3K) enzyme are required for β2AR-stimulated EGFR transactivation.
Lewis J, Watson +7 more
openaire +2 more sources
A microwave‐enhanced sustainable and versatile approach to substituted benzofurans from 2‐alkynylanisoles enabled by an active Brønsted acidic deep eutectic solvent. The research on alternative media for organic transformations remains a highly demanding topic.
Alessandra Gritti +9 more
wiley +1 more source
Alterations in vasodilator-stimulated phosphoprotein (VASP) phosphorylation: associations with asthmatic phenotype, airway inflammation and β\u3csub\u3e2\u3c/sub\u3e-agonist use [PDF]
Background Vasodilator-stimulated phosphoprotein (VASP) mediates focal adhesion, actin filament binding and polymerization in a variety of cells, thereby inhibiting cell movement.
Batra, Vikas +8 more
core +1 more source
Negative impact of β-arrestin-1 on post-myocardial infarction heart failure via cardiac and adrenal-dependent neurohormonal mechanisms [PDF]
β-Arrestin (βarr)-1 and β-arrestin-2 (βarrs) are universal G-protein-coupled receptor adapter proteins that negatively regulate cardiac β-adrenergic receptor (βAR) function via βAR desensitization and downregulation.
Bathgate Siryk, Ashley +11 more
core +1 more source
The beta-adrenergic receptor kinase (betaARK) is the prototypical member of the family of cytosolic kinases that phosphorylate guanine nucleotide binding-protein-coupled receptors and thereby trigger uncoupling between receptors and guanine nucleotide binding proteins.
R, Winstel +4 more
openaire +3 more sources

