Results 61 to 70 of about 37,687,396 (313)

The role of dimerisation in the cellular trafficking of G-protein-coupled receptors [PDF]

, 2010
The concept that G-protein-coupled receptors can exist as homomeric and/or heteromeric complexes is now well established. Despite this, how dynamic such interactions are and if this may be modulated during receptor trafficking remain topics of debate ...
Milligan, Graeme
core   +1 more source

Lipid-mediated Regulation of G Protein-coupled Receptor Kinases 2 and 3 [PDF]

Journal of Biological Chemistry, 1995
G protein-coupled receptor-mediated signaling is attenuated by a process referred to as desensitization, wherein agonist-dependent phosphorylation of receptors by G protein-coupled receptor kinases (GRKs) is proposed to be a key initial event. However, mechanisms that activate GRKs are not fully understood.
S K, DebBurman, J, Ptasienski, E, Boetticher, J W, Lomasney, J L, Benovic, M M, Hosey   +5 more
openaire   +2 more sources

Development of Inflammatory Immune Response-Related Drugs Based on G Protein-Coupled Receptor Kinase 2

Cellular Physiology and Biochemistry, 2018
G protein-coupled receptor kinase 2 (GRK2), as a vital Ser/Thr kinase, is an important regulatory protein in the inflammatory immune response (IIR) by maintaining the balance between the function of inflammatory immune cells and non-conventional ...
Chenchen Han, Yifan Li, Yang Wang, Dongqian Cui, Tingting Luo, Yuwen Zhang, Yang Ma, Wei  Wei   +7 more
doaj   +1 more source

Targeting cardiac beta-adrenergic signaling via GRK2 inhibition for heart failure therapy

Frontiers in Physiology, 2013
Cardiac cells, like those of the other tissues, undergo regulation through membrane-bound proteins known as G protein-coupled receptors (GPCRs). β-adrenergic receptors (βARs) are key GPCRs expressed on cardiomyocytes and their role is crucial in cardiac
Alessandro eCannavo, Daniela eLiccardo, Walter J. Koch   +2 more
doaj   +1 more source

Myocardial pathology induced by aldosterone is dependent on non-canonical activities of G protein-coupled receptor kinases

Nature Communications, 2016
High aldosterone levels cause heart damage independently of its well-known effect on blood pressure. Here, Cannavo et al. show that aldosterone-mediated cardiac pathology involves G protein-coupled receptor (GPCR) kinase 2 (GRK2) and GRK5 that integrate ...
Alessandro Cannavo, Daniela Liccardo, Akito Eguchi, Katherine J. Elliott, Christopher J. Traynham, Jessica Ibetti, Satoru Eguchi, Dario Leosco, Nicola Ferrara, Giuseppe Rengo, Walter J. Koch   +10 more
doaj   +1 more source

Skeletal muscle myogenesis is regulated by G protein-coupled receptor kinase 2 [PDF]

Journal of Molecular Cell Biology, 2014
G protein-coupled receptor kinase 2 (GRK2) is an important serine/threonine-kinase regulating different membrane receptors and intracellular proteins. Attenuation of Drosophila Gprk2 in embryos or adult flies induced a defective differentiation of somatic muscles, loss of fibers, and a flightless phenotype.
García-Guerra, Lucía, Vila-Bedmar, Rocío, Carrasco-Rando, Marta, Cruces-Sande, Marta, Martín-Martínez, Mercedes, Ruiz-Gómez, Ana, Ruiz-Gómez, Mar, Lorenzo, Margarita, Fernández-Veledo, Sonia, Mayor Menéndez, Federico, Murga, Cristina, Nieto-Vázquez, Iria   +11 more
openaire   +4 more sources

G protein-coupled receptor kinase 2 as a therapeutic target for heart failure [PDF]

Drug Discovery Today: Therapeutic Strategies, 2012
An ever-increasing number of people world-wide are developing and suffering from heart failure, and existing therapies, although improved are not ideal. Therefore, innovative treatment strategies are urgently needed. As our understanding of the underlying dysfunction of the myocardium increases, so does our ability to target the mechanisms responsible ...
Sarah M, Schumacher-Bass, Christopher J, Traynham, Walter J, Koch   +2 more
openaire   +2 more sources

G Protein-Coupled Receptor Kinase 2 Ablation in Cardiac Myocytes Before or After Myocardial Infarction Prevents Heart Failure

Circulation Research, 2008
Myocardial G protein-coupled receptor kinase (GRK)2 is a critical regulator of cardiac &bgr;-adrenergic receptor (&bgr;AR) signaling and cardiac function.
P. Raake, L. Vinge, E. Gao, M. Boucher, G. Rengo, Xiong-Wen Chen, B. DeGeorge, S. Matkovich, S. Houser, P. Most, A. Eckhart, G. Dorn, W. Koch   +12 more
semanticscholar   +1 more source

Agonist-dependent Phosphorylation of the G Protein-coupled Receptor Kinase 2 (GRK2) by Src Tyrosine Kinase*

Journal of Biological Chemistry, 1999
GRK2 is a member of the G protein-coupled receptor kinase (GRK) family, which phosphorylates the activated form of a variety of G protein-coupled receptors (GPCR) and plays an important role in GPCR modulation.
Susana Sarnago, Ana Elorza, F. Mayor
semanticscholar   +1 more source

Involvement of Intramolecular Interactions in the Regulation of G Protein-Coupled Receptor Kinase 2

Molecular Pharmacology, 2003
The G protein-coupled receptor (GPCR) kinase GRK2 phosphorylates G protein-coupled receptors in an agonist-dependent manner. GRK2 activity is modulated through interactions of diverse domains of the kinase with G protein betagamma subunits, several lipids, anchoring proteins, and activated receptors.
Susana, Sarnago, Ramón, Roca, Antonio, de Blasi, Alfonso, Valencia, Federico, Mayor, Cristina, Murga   +5 more
openaire   +2 more sources