EC Number | Inhibitors | Comment | Organism | Structure |
---|---|---|---|---|
2.7.11.15 | GRK2ct | GRK2 inhibitor GRK2ct corresponding to the carboxyl-terminal 194 amino acids of GRK2 is expressed in failing cardiac fibroblasts using an adenoviral-mediated approach driven by the CMV promoter. Inhibition restores beta-agonist stimulated inhibition of collagen synthesis and decreases collagen synthesis in response to TGF beta stimulation | Homo sapiens |
EC Number | Organism | UniProt | Comment | Textmining |
---|---|---|---|---|
2.7.11.15 | Homo sapiens | - |
- |
- |
EC Number | Source Tissue | Comment | Organism | Textmining |
---|---|---|---|---|
2.7.11.15 | fibroblast | - |
Homo sapiens | - |
EC Number | Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|---|
2.7.11.15 | ATP + rhodopsin | - |
Homo sapiens | ADP + phosphorylated rhodopsin | - |
? |
EC Number | Synonyms | Comment | Organism |
---|---|---|---|
2.7.11.15 | GRK2 | - |
Homo sapiens |
EC Number | Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|---|
2.7.11.15 | 20 | - |
assay at | Homo sapiens |
EC Number | pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|---|
2.7.11.15 | 7.5 | - |
assay at | Homo sapiens |
EC Number | Organism | Comment | Expression |
---|---|---|---|
2.7.11.15 | Homo sapiens | a 4fold increase in GRK2 expression in the failing cardiac fibroblasts is detected compared with normal controls | up |
EC Number | General Information | Comment | Organism |
---|---|---|---|
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 | Homo sapiens |
2.7.11.15 | physiological function | GRK2 plays a significant role in regulating collagen synthesis in adult human cardiac fibroblasts | Homo sapiens |