- Protein Name
- Beta-adrenergic receptor kinase 1
- Gene Name
- GRK2
- Organism
-
Homo sapiens
- Function
- Specifically phosphorylates the agonist-occupied form of the beta-adrenergic and closely related receptors, probably inducing a desensitization of them. Key regulator of LPAR1 signaling. Competes with RALA for binding to LPAR1 thus affecting the signaling properties of the receptor. Desensitizes LPAR1 and LPAR2 in a phosphorylation-independent manner.
| Site |
Maximum Consensus Site Population |
Minimum Consensus Site Population |
Median Consensus Site Population |
| MPP |
13 |
13 |
13.0 |
| DFG |
25 |
4 |
14.5 |
| DRS |
18 |
10 |
14.0 |
| EDI |
19 |
4 |
12.0 |
| MT3 |
6 |
5 |
5.5 |
| AAS |
15 |
3 |
5.0 |
| LBP |
3 |
3 |
3.0 |
| CMP |
11 |
2 |
8.0 |
| PDIG |
2 |
2 |
2.0 |
| ATP |
17 |
4 |
16.0 |
| PMP |
2 |
2 |
2.0 |
| PDB ID |
Maximum Consensus Site Population |
| MPP site |
DFG site |
PIF site |
DRS site |
DEF site |
EDI site |
MT3 site |
AAS site |
LBP site |
CMP site |
PDIG site |
ATP site |
PMP site |
| Total Druggable Structures per Site |
0 |
4 |
0 |
3 |
0 |
1 |
0 |
0 |
0 |
0 |
0 |
5 |
0 |
|
4PNK
|
0 |
22 |
0 |
18 |
0 |
0 |
0 |
3 |
0 |
6 |
0 |
16 |
2 |
|
3V5W
|
0 |
21 |
0 |
14 |
0 |
0 |
6 |
9 |
0 |
2 |
0 |
16 |
0 |
|
4MK0
|
0 |
10 |
0 |
16 |
0 |
0 |
0 |
15 |
0 |
10 |
2 |
15 |
0 |
|
5HE1
|
0 |
4 |
0 |
16 |
0 |
4 |
5 |
5 |
0 |
8 |
0 |
15 |
0 |
|
3KRX
|
0 |
9 |
0 |
10 |
0 |
0 |
0 |
0 |
0 |
0 |
0 |
17 |
0 |
|
3CIK
|
0 |
25 |
0 |
13 |
0 |
19 |
0 |
0 |
0 |
0 |
0 |
17 |
0 |
|
AFP25098
|
13 |
0 |
0 |
0 |
0 |
0 |
0 |
0 |
0 |
0 |
0 |
0 |
0 |
|
3KRW
|
0 |
19 |
0 |
12 |
0 |
12 |
0 |
4 |
3 |
11 |
0 |
17 |
0 |