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Literature summary for 2.7.11.16 extracted from

  • Willets, J.M.; Mistry, R.; Nahorski, S.R.; Challiss, R.A.
    Specificity of G protein-coupled receptor kinase 6-mediated phosphorylation and regulation of single-cell M3 muscarinic acetylcholine receptor signaling (2003), Mol. Pharmacol., 64, 1059-1068.
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
methacholine stimulation of M3 muscarinic acetylcholine receptor phosphorylation is reversible by atropine Homo sapiens
additional information GRK6 activity on the M3 muscarinic acetylcholine receptor is not affected by phorbol-12,13-dibutyrate and Ro 31-8220 Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
stable overexpression of wild-type and K215R mutant GRK6 in SH-SY5Y neuroblastoma cells via adenovirus infection system Homo sapiens

Protein Variants

Protein Variants Comment Organism
K215R site-directed mutagenesis, inactive, dominant negative mutant of GRK6, 30fold overexpression in SH-SY5Y cells produces a 50% suppression of endogenous M3 muscarinic acetylcholine receptor phosphorylation and desensitization by the wild-type enzyme, GRK5 K215R mutant overexpression has no effect Homo sapiens
additional information overexpression of wild-type GRK6 increase the endogenous M3 muscarinic acetylcholine receptor phosphorylation and desensitization level Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
additional information GRK6 activity on the M3 muscarinic acetylcholine receptor is not affected by phorbol-12,13-dibutyrate and Ro 31-8220 Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+
-
Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + [M3 muscarinic acetylcholine receptor] Homo sapiens GRK6 plays a major role in specific M3 muscarinic acetylcholine receptor regulation ADP + phospho-[M3 muscarinic acetylcholine receptor]
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
SH-SY5Y cell neuroblastoma cell line, contains no GRK5 Homo sapiens
-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
additional information
-
-
Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + [M3 muscarinic acetylcholine receptor]
-
Homo sapiens ADP + phospho-[M3 muscarinic acetylcholine receptor]
-
?
ATP + [M3 muscarinic acetylcholine receptor] GRK6 plays a major role in specific M3 muscarinic acetylcholine receptor regulation Homo sapiens ADP + phospho-[M3 muscarinic acetylcholine receptor]
-
?

Synonyms

Synonyms Comment Organism
G protein-coupled receptor kinase 6
-
Homo sapiens
GRK6
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
assay at Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
Homo sapiens