Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 2.7.11.15 extracted from

  • Fernandez, N.; Gottardo, F.L.; Alonso, M.N.; Monczor, F.; Shayo, C.; Davio, C.
    Roles of phosphorylation-dependent and -independent mechanisms in the regulation of histamine H2 receptor by G protein-coupled receptor kinase 2 (2011), J. Biol. Chem., 286, 28697-28706.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.7.11.15

Cloned(Commentary)

Cloned (Comment) Organism
expresed in HEK293T cells and COS7 cells Bos taurus

Protein Variants

Protein Variants Comment Organism
D110A the expression of the D110A mutant in COS7-transfected cells fails to desensitize the histamine H2 receptor Bos taurus
D110A/K220R double mutant has a disrupted RGS (regulator of G protein signalling) function. Although double mutant coimmunoprecipitates with the histamine H2 receptor, it reverses GRK2K220R-mediated histamine H2 receptor desensitization Bos taurus
K220R catalytically inactive mutant. Mutant cells desensitize histamine H2 receptor signaling in the same degree as the GRK2 wild type cells. Although the receptor phosphorylation is crucial for histamine H2 receptor internalization and resensitization, the kinase activity is not required to achieve histamine H2 receptor desensitization Bos taurus
additional information to identify the domains responsible for the kinase-independent receptor desensitization, the histamine H2 receptor is co-transfected with constructions encoding the GRK2 RGS-homology domain (RH) and the RH or the kinase domain fused to the pleckstrin homology domain. Results demonstrate that the RH domain of GRK2 is sufficient to desensitize the histamine H2 receptor Bos taurus

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
histamine H2 receptor + ATP Bos taurus
-
 phosphorylated histamine H2 receptor + ADP
-
 ?

Organism

Organism UniProt Comment Textmining
Bos taurus
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
histamine H2 receptor + ATP
-
 Bos taurus phosphorylated histamine H2 receptor + ADP
-
 ?

Synonyms

Synonyms Comment Organism
GRK2
-
 Bos taurus

General Information

General Information Comment Organism
malfunction GRK2 kinase activity and, therefore, histamine H2 receptor phosphorylation, is required to achieve H2R internalization but not receptor desensitization Bos taurus