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Literature summary for 2.7.11.15 extracted from

  • Willets, J.M.; Nahorski, S.R.; Challiss, R.A.
    Roles of phosphorylation-dependent and -independent mechanisms in the regulation of M1 muscarinic acetylcholine receptors by G protein-coupled receptor kinase 2 in hippocampal neurons (2005), J. Biol. Chem., 280, 18950-18958.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
co-expression of HA-tagged M1 muscarinic acetylcholine receptor and of GRK2 wild-type and mutants in CHO-K1 cells, suppression of 80% of endogenous GRK2 in HEK293 cells and in hippocampal neurons by antisense construct expression of GRK2, co-expression of wild-type and mutant GRK2s with eGFP-tagged inositol 1,4,5-trisphosphate biosensor eGFP-PHPLCdelta in HEK293 cells Rattus norvegicus

Protein Variants

Protein Variants Comment Organism
D110A site-directed mutagenesis, GRK2 mutant deficient in Galphaq/11 binding Rattus norvegicus
D110A/K220R site-directed mutagenesis, inactive GRK2 mutant deficient in Galphaq/11 binding Rattus norvegicus
K220R site-directed mutagenesis, inactive mutant GRK2 Rattus norvegicus
additional information construction of GRK2-depleted hippocampal neurons and expression of a GRK2 mutant deficient in Galphaq/11 binding, overexpression of eGFP-tagged inositol 1,4,5-trisphosphate biosensor eGFP-PHPLCdelta leads to suppression of M1 muscarinic acetylcholine receptor-mediated phospholipase C signaling in hippocampal neurons through a phosphorylation-independent mechanism via binding of Galphaq/11 to the RGS homology domain of the enzyme Rattus norvegicus

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + M1 muscarinic acetylcholine receptor Rattus norvegicus phosphorylation-dependent and -independent mechanisms in the regulation of M1 muscarinic acetylcholine receptors by G protein-coupled receptor kinase 2 in hippocampal neurons, GRK2 can inhibit the receptor-dependent signaling via phospholipase C, overview ADP + phosphorylated M1 muscarinic acetylcholine receptor
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Organism

Organism UniProt Comment Textmining
Rattus norvegicus
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-
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Source Tissue

Source Tissue Comment Organism Textmining
hippocampus
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Rattus norvegicus
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neuron hippocampal Rattus norvegicus
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Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
additional information
-
-
Rattus norvegicus

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + M1 muscarinic acetylcholine receptor
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Rattus norvegicus ADP + phosphorylated M1 muscarinic acetylcholine receptor
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ATP + M1 muscarinic acetylcholine receptor phosphorylation-dependent and -independent mechanisms in the regulation of M1 muscarinic acetylcholine receptors by G protein-coupled receptor kinase 2 in hippocampal neurons, GRK2 can inhibit the receptor-dependent signaling via phospholipase C, overview Rattus norvegicus ADP + phosphorylated M1 muscarinic acetylcholine receptor
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Synonyms

Synonyms Comment Organism
G protein-coupled receptor kinase 2
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Rattus norvegicus
GRK2
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Rattus norvegicus

Cofactor

Cofactor Comment Organism Structure
ATP
-
Rattus norvegicus