Results 31 to 40 of about 6,551 (208)
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
Inhibition of the G-protein-coupled receptor kinase 2 (GRK2) is an emerging treatment approach for heart failure. Therefore, cardio-protective mechanisms induced by GRK2 inhibition are under investigation. We compared two different GRK2 inhibitors, i.e.,
Stefan Wolf +3 more
doaj +1 more source
G protein-coupled receptor kinase 2 promotes cardiac hypertrophy.
The increase in protein activity and upregulation of G-protein coupled receptor kinase 2 (GRK2) is a hallmark of cardiac stress and heart failure. Inhibition of GRK2 improved cardiac function and survival and diminished cardiac remodeling in various ...
Philipp Schlegel +12 more
doaj +1 more source
G protein‐coupled receptor (GPCR) kinases (GRKs) were identified by their ability to phosphorylate activated GPCRs. They constitute a branch of the AGC kinase superfamily and are activated by hormone‐treated receptors. Their mechanism of activation is largely unknown; thus, we initiated a study to identify GRK2
Rachel Sterne‐Marr +5 more
openaire +1 more source
The Metabolic Role of GRK2 in Insulin Resistance and Associated Conditions [PDF]
Insulin resistance (IRES) is a pathophysiological condition characterized by the reduced response to insulin of several tissues, including myocardial and skeletal muscle. IRES is associated with obesity, glucose intolerance, dyslipidemia, and hypertension, evolves toward type 2 diabetes, and increases the risk of developing cardiovascular diseases ...
Daniela Sorriento +7 more
openaire +5 more sources
Regulation of GPR54 Signaling by GRK2 and β-Arrestin [PDF]
AbstractKisspeptin and its receptor, GPR54, are major regulators of the hypothalamic-pituitary-gonadal axis as well as regulators of human placentation and tumor metastases. GPR54 is a Gq/11-coupled G protein-coupled receptor (GPCR), and activation by kisspeptin stimulates phosphatidy linositol 4, 5-biphosphate hydrolysis, Ca2+ mobilization ...
Macarena, Pampillo +8 more
openaire +2 more sources
Background: Identification of signaling pathways altered at early stages after cardiac ischemia/reperfusion (I/R) is crucial to develop timely therapies aimed at reducing I/R injury.
Petronila Penela +5 more
doaj +1 more source
The timing of centrosome separation and the distance moved apart influence the formation of the bipolar spindle, affecting chromosome stability. Epidermal growth factor receptor (EGFR) signaling induces early centrosome separation through downstream G ...
Clara Reglero +4 more
doaj +1 more source
Phosphoproteomic-based kinase profiling early in influenza virus infection identifies GRK2 as antiviral drug target. [PDF]
Although annual influenza epidemics affect around 10% of the global population, current treatment options are limited and development of new antivirals is needed.
Hunziker, Annika +12 more
core +2 more sources
GRK2-Dependent HuR Phosphorylation Regulates HIF1α Activation under Hypoxia or Adrenergic Stress [PDF]
© 2020 by the authors.Adaptation to hypoxia is a common feature in solid tumors orchestrated by oxygen-dependent and independent upregulation of the hypoxia-inducible factor-1α (HIF-1α). We unveiled that G protein-coupled receptor kinase (GRK2), known to
Tapia, Olga +31 more
core +1 more source

