Cloned (Comment) | Organism |
---|---|
expresed in HEK293T cells and COS7 cells | Bos taurus |
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 | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
histamine H2 receptor + ATP | Bos taurus | - |
phosphorylated histamine H2 receptor + ADP | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Bos taurus | - |
- |
- |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
histamine H2 receptor + ATP | - |
Bos taurus | phosphorylated histamine H2 receptor + ADP | - |
? |
Synonyms | Comment | Organism |
---|---|---|
GRK2 | - |
Bos taurus |
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 |