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Literature summary for 2.7.11.15 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
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Inhibitors

Inhibitors Comment Organism Structure
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

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
fibroblast
-
 Homo sapiens
-

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
GRK2
-
 Homo sapiens

Temperature Optimum [°C]

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

pH Optimum

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

Expression

Organism Comment Expression
Homo sapiens a 4fold increase in GRK2 expression in the failing cardiac fibroblasts is detected compared with normal controls up

General Information

General Information Comment Organism
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
physiological function GRK2 plays a significant role in regulating collagen synthesis in adult human cardiac fibroblasts Homo sapiens