Results 21 to 30 of about 9,380 (213)
GRK2 in the Heart: A GPCR Kinase and Beyond [PDF]
Significance: Heart failure (HF) is a common end point for many underlying cardiovascular diseases. Down-regulation and desensitization of β-adrenergic receptors (β-AR) caused by G-protein-coupled receptor (GPCR) kinase 2 (GRK2) are prominent features of HF.
Zheng Maggie, Huang +3 more
openaire +2 more sources
Characterization of the GRK2 Binding Site of Gαq [PDF]
Heterotrimeric guanine nucleotide-binding proteins (G proteins) transmit signals from membrane bound G protein-coupled receptors (GPCRs) to intracellular effector proteins. The G(q) subfamily of Galpha subunits couples GPCR activation to the enzymatic activity of phospholipase C-beta (PLC-beta).
Peter W, Day +5 more
openaire +2 more sources
G protein-coupled receptor kinase 2 (GRK2) is an adapter protein that modulates G protein-coupled receptor (GPCR) signaling. It also regulates the functions and activity of other intracellular proteins in many cell types.
Ananth K. Kammala +4 more
doaj +1 more source
Cardiovascular disease (CVD) risk shows a clear sexual dimorphism with age, with a lower incidence in young women compared to age-matched men. However, this protection is lost after menopause. We demonstrate that sex-biased sensitivity to the development
Alba C. Arcones +7 more
doaj +1 more source
Trafficking GRK2: Cellular and Metabolic consequences of GRK2 subcellular localization.
G protein coupled receptor kinase 2 (GRK2) has a key role in cellular function by regulating different intracellular mechanisms in a kinase dependent or independent manner. In this review we have dealt with the recently discovered roles of GRK2 in the regulation of cell metabolism.
SORRIENTO, DANIELA +5 more
openaire +6 more sources
The RAF Kinase Inhibitor Protein (RKIP): Good as Tumour Suppressor, Bad for the Heart
The RAF kinase inhibitor protein, RKIP, is a dual inhibitor of the RAF1 kinase and the G protein-coupled receptor kinase 2, GRK2. By inhibition of the RAF1-MAPK (mitogen-activated protein kinase) pathway, RKIP acts as a beneficial tumour suppressor.
Joshua Abd Alla, Ursula Quitterer
doaj +1 more source
Tailoring therapy for heart failure: the pharmacogenomics of adrenergic receptor signaling. [PDF]
Heart failure is one of the leading causes of mortality in Western countries, and β-blockers are a cornerstone of its treatment. However, the response to these drugs is variable among individuals, which might be explained, at least in part, by genetic ...
Barrese, V +3 more
core +2 more sources
P440Targeting subcellular GRK2 localization [PDF]
GRK2 is a kinase involved in the regulation of G protein coupled receptor signaling and in particular phosphorylates beta adrenergic receptors at plasma membrane leading to desensitization. In animal and human models of heart failure, its increased level and activity are associated with a worse prognosis.
A Anastasio +5 more
openaire +1 more source
Novel inhibitors of phosphorylation independent activity of GRK2 modulate cAMP signaling
G protein‐coupled receptors kinase 2 (GRK2) plays a major role in receptor regulation and, as a consequence, in cell biology and physiology. GRK2‐mediated receptor desensitization is performed by its kinase domain, which exerts receptor phosphorylation ...
Emiliana Echeverría +5 more
doaj +1 more source
G protein-coupled receptor kinase-2 (GRK-2) regulates serotonin metabolism through the monoamine oxidase AMX-2 in Caenorhabditis elegans. [PDF]
G protein-coupled receptors (GPCRs) regulate many animal behaviors. GPCR signaling is mediated by agonist-promoted interactions of GPCRs with heterotrimeric G proteins, GPCR kinases (GRKs), and arrestins.
Aryal, Dipendra K. +5 more
core +2 more sources

