Results 21 to 30 of about 6,839 (207)
Novel inhibitors of phosphorylation independent activity of GRK2 modulate cAMP signaling
Pharmacology Research & Perspectives, 2022 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
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Canonical and Non-Canonical Roles of GRK2 in Lymphocytes
Cells, 2021 G protein-coupled receptor kinase 2 (GRK2) is emerging as a key integrative signaling node in a variety of biological processes ranging from cell growth and proliferation to migration and chemotaxis.
Jing Cheng +2 more
doaj +1 more source
GRK2 regulates GLP-1R-mediated early phase insulin secretion in vivo
BMC Biology, 2021 Background Insulin secretion from the pancreatic β-cell is finely modulated by different signals to allow an adequate control of glucose homeostasis.
Alba C. Arcones +8 more
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Cells, 2021 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
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Inhibition of WNT Signaling by G Protein-Coupled Receptor (GPCR) Kinase 2 (GRK2) [PDF]
Molecular Endocrinology, 2009 Activation of Wnt signaling pathways causes release and stabilization of the transcription regulator beta-catenin from a destruction complex composed of axin and the adenomatous polyposis coli (APC) protein (canonical signaling pathway). Assembly of this complex is facilitated by a protein-protein interaction between APC and a regulator of G protein ...
Liming, Wang +3 more
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Potent, Selective, and Drug-Like G Protein-Coupled Receptor Kinase 5 and 6 Inhibitors: Design, Synthesis, and X-Ray Structural Studies. [PDF]
ChemMedChemHerein, X‐ray structure‐based design, synthesis, and evaluation of a series of potent and selective small molecules G protein‐coupled receptor kinase 5 (GRK5) and GRK6 inhibitors that exhibit high selectivity against GRK2 are reported. A high‐resolution X‐ray crystal structure of GRK5 and inhibitor 6t complex provides important molecular insight for ...
Ghosh AK +5 more
europepmc +2 more sources
New roles of G protein-coupled receptor kinase 2 (GRK2) in cell migration [PDF]
Cell Adhesion & Migration, 2009 G protein-coupled receptor kinase 2 (GRK2) was initially identified as a key player, together with beta-arrestins, in the regulation of multiple G protein-coupled receptors (GPCR). Further research has revealed a complex GRK2 interactome, that includes a variety of proteins related to cell motility, and a role for GRK2 kinase activity in inhibiting ...
Penela, Petronila +3 more
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Regulation of Constitutive GPR3 Signaling and Surface Localization by GRK2 and β-arrestin-2 Overexpression in HEK293 Cells. [PDF]
PLoS ONE, 2013 G protein-coupled receptor 3 (GPR3) is a constitutively active receptor that maintains high 3'-5'-cyclic adenosine monophosphate (cAMP) levels required for meiotic arrest in oocytes and CNS function.
Katie M Lowther +4 more
doaj +1 more source
Acta Pharmaceutica Sinica B, 2021 Rheumatoid arthritis (RA) is an autoimmune disease and is mainly characterized by abnormal proliferation of fibroblast-like synoviocytes (FLS). The up-regulated cellular membrane expression of G protein coupled receptor kinase 2 (GRK2) of FLS plays a ...
Chenchen Han +12 more
doaj +1 more source
Agonist-dependent Phosphorylation of the G Protein-coupled Receptor Kinase 2 (GRK2) by Src Tyrosine Kinase [PDF]
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. It has been recently reported that stimulation of the mitogen-activated protein kinase cascade by GPCRs involves tyrosine phosphorylation of ...
S, Sarnago, A, Elorza, F, Mayor
openaire +2 more sources