EC Number   |
General Information |
Reference |
|---|
   2.7.11.15 | malfunction |
decreased enzyme expression in endothelial cells accelerates tumor growth in mice by impairing the pericytes ensheathing the vessels, thereby promoting hypoxia and macrophage infiltration |
739060 |
| 2.7.11.15 | malfunction |
enzyme ablation leads to marked vascular malformations involving impaired recruitment of mural cells. Enzyme downregulation is a relevant event in the tumoral angiogenic switch |
738755 |
| 2.7.11.15 | malfunction |
GRK2 kinase activity and, therefore, histamine H2 receptor phosphorylation, is required to achieve H2R internalization but not receptor desensitization |
725436 |
| 2.7.11.15 | malfunction |
morpholino silencing of the zebrafish ortholog of Gprk2 in fish embryos causes impaired cytokine expression after Escherichia coli infection |
725634 |
| 2.7.11.15 | malfunction |
overexpression of GRK2 in normal cardiac fibroblasts recapitulates a heart failure phenotype with minimal inhibition of collagen synthesis following beta-agonist stimulation. Knockdown of GRK2 expression in normal cardiac fibroblasts enhances cAMP production and leads to greater beta-agonist-mediated inhibition of basal and TGF beta-stimulated collagen synthesis versus control. Inhibition of GRK2 activity in failing cardiac fibroblasts by expression of the GRK2 inhibitor, GRK2ct, or siRNA-mediated knockdown restores beta-agonist stimulated inhibition of collagen synthesis and decreases collagen synthesis in response to TGF beta stimulation |
725420 |
| 2.7.11.15 | malfunction |
RNA silencing of GRK5 in HeLa cells impairs NF-kappaB reporter activity |
725634 |
| 2.7.11.15 | malfunction |
the influence of GRK2 levels is investigated in insulin signaling in myoblasts and adipocytes with experimentally increased or silenced levels of GRK2, as well as in GRK2 hemizygous animals expressing 50% lower levels of this kinase in three different models of insulin resistance: TNF-alpha infusion, aging, and high-fat diet (HFD). GRK2 levels are increased by 2fold in muscle and adipose tissue in the animal models tested. In contrast, hemizygous GRK2 mice show enhanced insulin sensitivity and do not develop insulin resistance by TNF-alpha, aging, or high-fat diet. Reduced GRK2 levels induce a lean phenotype and decrease age-related adiposity |
724817 |
| 2.7.11.15 | malfunction |
transgenic mice with cardiac-specific overexpression of GRK2 negatively impact cardiac metabolism by inhibiting glucose uptake and desensitization of insulin signaling, which increases after ischemic injury and precedes heart failure development. Mechanistically, GRK2 interacts with and directly phosphorylates insulin receptor substrate-1 (IRS1) in cardiomyocytes causing insulin-dependent negative signaling feedback including inhibition of membrane translocation of the glucose transporter, GLUT4 |
724780 |
| 2.7.11.15 | malfunction |
using a genome-wide RNAi screen Grk2 is identified as a conserved regulator of NF-kappaB signaling |
725634 |
| 2.7.11.15 | malfunction |
using gprk2 mutant flies its shown that G-protein-coupled receptor kinase 2 regulates cAMP-dependent Hedgehog signaling |
724816 |
