Results 11 to 20 of about 37,687,396 (313)

Regulation of G protein-coupled receptor kinase 2 and its role in tumors [PDF]

Journal of Translational Medicine
Background G protein-coupled receptor kinase 2(GRK2) is a pivotal regulator of G protein-coupled receptor (GPCR) signal desensitization. It is increasingly recognized for its involvement in the pathogenesis of various malignancies through non-canonical ...
Chenmin Liu, Liuli Yang, Shiyu Peng, Jiangbo Jing, Lijuan Ma   +4 more
doaj   +4 more sources

G protein-coupled receptor kinase 2-mediated phosphorylation of ezrin is required for G protein-coupled receptor-dependent reorganization of the actin cytoskeleton. [PDF]

Molecular Biology of the Cell, 2005
G protein-coupled receptor kinase 2 (GRK2) phosphorylates and desensitizes activated G protein-coupled receptors (GPCRs). Here, we identify ezrin as a novel non-GPCR substrate of GRK2. GRK2 phosphorylates glutathione S-transferase (GST)-ezrin, but not an ezrin fusion protein lacking threonine 567 (T567), in vitro.
S. H. Cant, J. Pitcher
semanticscholar   +6 more sources

Aldosterone Jeopardizes Myocardial Insulin and β-Adrenergic Receptor Signaling via G Protein-Coupled Receptor Kinase 2 [PDF]

Frontiers in Pharmacology, 2019
Hyperaldosteronism alters cardiac function, inducing adverse left ventricle (LV) remodeling either via increased fibrosis deposition, mitochondrial dysfunction, or both.
Alessandro Cannavo, Alessandro Cannavo, Federica Marzano, Andrea Elia, Daniela Liccardo, Leonardo Bencivenga, Giuseppina Gambino, Claudia Perna, Antonio Rapacciuolo, Antonio Cittadini, Nicola Ferrara, Nicola Ferrara, Nazareno Paolocci, Nazareno Paolocci, Walter J. Koch, Giuseppe Rengo, Giuseppe Rengo   +16 more
doaj   +2 more sources

G-Protein-Coupled Receptor Kinase 2 Limits CCL21-Induced T Cell Migration via Phospholipase Cγ1 [PDF]

Receptors
Background/Objectives: G protein-coupled receptors (GPCRs) can promote ligand-biased signaling, yet the mechanisms that promote bias are not well understood.
Anahi Sanchez, Caitlin T. Winebrenner, Natalia Garcia, Brian Kaiser, Lyndsey Kilgore, Cesar I. Cardona, Daniel W. Bassuk, Mary E. Miller, Charles A. Bill, Laura A. Shannon, Brant M. Wagener, Amy Wagler, Manuel Llano, Colin A. Bill, Charlotte M. Vines   +14 more
doaj   +2 more sources

G protein-coupled receptor kinase 2 promotes flaviviridae entry and replication. [PDF]

PLoS Neglected Tropical Diseases, 2012
Flaviviruses cause a wide range of severe diseases ranging from encephalitis to hemorrhagic fever. Discovery of host factors that regulate the fate of flaviviruses in infected cells could provide insight into the molecular mechanisms of infection and ...
Caroline Le Sommer, Nicholas J Barrows, Shelton S Bradrick, James L Pearson, Mariano A Garcia-Blanco   +4 more
doaj   +4 more sources

Structure-Based Design of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors Based on Paroxetine. [PDF]

J Med Chem, 2017
In heart failure, the β-adrenergic receptors (βARs) become desensitized and uncoupled from heterotrimeric G proteins. This process is initiated by G protein-coupled receptor kinases (GRKs), some of which are upregulated in the failing heart making them ...
Waldschmidt HV, Homan KT, Cato MC, Cruz-Rodríguez O, Cannavo A, Wilson MW, Song J, Cheung JY, Koch WJ, Tesmer JJ, Larsen SD.   +10 more
europepmc   +2 more sources

G protein-coupled receptor kinase-2: A potential biomarker for early diabetic cardiomyopathy. [PDF]

J Diabetes, 2020
G protein‐coupled receptor kinase‐2 (GRK2) has been shown as a key regulator of cardiac function, and the myocardial GRK2 levels are mirrored by the levels in peripheral blood mononuclear cells (PBMCs).
Lai S, Fu X, Yang S, Zhang S, Lin Q, Zhang M, Chen H.   +6 more
europepmc   +2 more sources

Degradation of the G Protein-coupled Receptor Kinase 2 by the Proteasome Pathway* [PDF]

Journal of Biological Chemistry, 1998
GRK2 is a ubiquitous member of the G protein-coupled receptor kinase (GRK) family and has been shown to play a key role in determining the desensitization and resensitization patterns of a variety of G protein-coupled receptors.
P. Penela, A. Ruiz-Gómez, J. Castaño, F. Mayor   +3 more
semanticscholar   +3 more sources

Obesity-induced cardiac lipid accumulation in adult mice is modulated by G protein-coupled receptor kinase 2 levels. [PDF]

Cardiovasc Diabetol, 2016
BackgroundThe leading cause of death among the obese population is heart failure and stroke prompted by structural and functional changes in the heart.
Lucas E, Vila-Bedmar R, Arcones AC, Cruces-Sande M, Cachofeiro V, Mayor F, Murga C.   +6 more
europepmc   +2 more sources

Structure-Based Design, Synthesis, and Biological Evaluation of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors. [PDF]

J Med Chem, 2016
G protein-coupled receptors (GPCRs) are central to many physiological processes. Regulation of this superfamily of receptors is controlled by GPCR kinases (GRKs), some of which have been implicated in heart failure.
Waldschmidt HV, Homan KT, Cruz-Rodríguez O, Cato MC, Waninger-Saroni J, Larimore KM, Cannavo A, Song J, Cheung JY, Kirchhoff PD, Koch WJ, Tesmer JJ, Larsen SD.   +12 more
europepmc   +2 more sources