Results 71 to 80 of about 28,675 (270)

Mapping the druggable allosteric space of G-protein coupled receptors: a fragment-based molecular dynamics approach. [PDF]

, 2010
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

Drugs induced Raynaud's phenomenon and underlying mechanism: a disproportionality analysis from the WHO pharmacovigilance database

Arthritis &Rheumatology, Accepted Article.
Objectives The aim of this study is to generate hypotheses about unknown drugs associated with the onset or worsening of Raynaud's Phenomenon (RP) and to explore their potential pathophysiological mechanisms through a mixed disproportionality/clustering analysis from the WHO pharmacovigilance database.
Alex Hlavaty, Loubna Dari, Jean‐Luc Cracowski, Matthieu Roustit, Charles Khouri   +4 more
wiley   +1 more source

Contribution of the sympathetic nervous system to the pathogenesis of salt-sensitive hypertension [PDF]

, 2016
Dysregulation of the sodium-chloride cotransporter (NCC) is believed to significantly impact blood pressure. Recent studies have implicated overactivity of the sympathetic nervous system as a mechanism driving renal NCC dysregulation to evoke the ...
Pazzol, Michael Lee
core   +1 more source

Downregulation of G protein-coupled receptor kinase 2 levels enhances cardiac insulin sensitivity and switches on cardioprotective gene expression patterns [PDF]

, 2016
© 2014 Elsevier B.V. G protein-coupled receptor kinase 2 (GRK2) has recently emerged as a negative modulator of insulin signaling. GRK2 downregulation improves insulin sensitivity and prevents systemic insulin resistance.
Jurado-Pueyo, María, Lucas, Elisa, Mayor Menéndez, Federico, Murga, Cristina, Vila-Bedmar, Rocío   +4 more
core   +1 more source

Systemic aging fuels heart failure: Molecular mechanisms and therapeutic avenues

ESC Heart Failure, Volume 12, Issue 2, Page 1059-1080, April 2025.
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, Umar Raza, Jia Song, Junyan Lu, Shun Yao, Xiaohong Liu, Wei Zhang, Shujuan Li   +7 more
wiley   +1 more source

The β-Adrenergic Receptor Kinase (GRK2) Is Regulated by Phospholipids [PDF]

Journal of Biological Chemistry, 1995
The beta-adrenergic receptor kinase (beta ARK) is a member of growing family of G protein coupled receptor kinases (GRKs). beta ARK and other members of the GRK family play a role in the mechanism of agonist-specific desensitization by virtue of their ability to phosphorylate G protein-coupled receptors in an agonist-dependent manner.
J J, Onorato, M E, Gillis, Y, Liu, J L, Benovic, A E, Ruoho   +4 more
openaire   +2 more sources

Semaglutide normalizes increased cardiomyocyte calcium transients in a rat model of high fat diet‐induced obesity

ESC Heart Failure, Volume 12, Issue 2, Page 1386-1397, April 2025.
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, Julia Theisen, Katharina J. Ermer, Marie Oertel, Anton Xu, David Weissman, Katharina Ecker, Jan Dudek, Martin Fassnacht, Alexander Nickel, Michael Kohlhaas, Christoph Maack, Ulrich Dischinger   +12 more
wiley   +1 more source

GRK et arrestines : la piste thérapeutique ? [PDF]

, 2006
La phosphorylation d’un récepteur couplé aux protéines G (RCPG) par une kinase spécifique, nommée GRK (G protein-coupled receptor kinase), est une première étape qui participe, avec l’action des arrestines, à l’arrêt de la transmission du signal, au ...
Kraimps, Jean-Louis, Métayé, Thierry, Perdrisot, Rémy   +2 more
core   +1 more source

Cilostazol in patients with heart failure and preserved ejection fraction—The CLIP‐HFpEF trial

ESC Heart Failure, Volume 12, Issue 2, Page 1437-1446, April 2025.
• 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, Jeanne du Fay de Lavallaz, Michael J. Zhang, Thanat Chaikijurajai, Bo Ye, Prabhjot S. Nijjar, Julie A. Lahiri, Cindy M. Martin, Tamas Alexy, Markus Meyer   +9 more
wiley   +1 more source

Nanodelivery of a functional membrane receptor to manipulate cellular phenotype. [PDF]

, 2018
Modification of membrane receptor makeup is one of the most efficient ways to control input-output signals but is usually achieved by expressing DNA or RNA-encoded proteins or by using other genome-editing methods, which can be technically challenging ...
Baikoghli, Mo, Cheng, R Holland, Coleman, Matthew A, He, Wei, Patriarchi, Tommaso, Shen, Ao, Tian, Lin, Xiang, Yang K   +7 more
core   +2 more sources