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Literature summary extracted from

  • DSouza, K.M.; Malhotra, R.; Philip, J.L.; Staron, M.L.; Theccanat, T.; Jeevanandam, V.; Akhter, S.A.
    G protein-coupled receptor kinase-2 is a novel regulator of collagen synthesis in adult human cardiac fibroblasts (2011), J. Biol. Chem., 286, 15507-15516.
    View publication on PubMedView publication on EuropePMC

Inhibitors

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

Organism

EC Number Organism UniProt Comment Textmining
2.7.11.15 Homo sapiens
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.7.11.15 fibroblast
-
Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.11.15 ATP + rhodopsin
-
Homo sapiens ADP + phosphorylated rhodopsin
-
?

Synonyms

EC Number Synonyms Comment Organism
2.7.11.15 GRK2
-
Homo sapiens

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
2.7.11.15 20
-
assay at Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
2.7.11.15 7.5
-
assay at Homo sapiens

Expression

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

General Information

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