Nomenclature
Short Name:
GRK7
Full Name:
G protein-coupled receptor kinase 7
Alias:
- EC 2.7.1.-
- EC 2.7.11.16
- GPRK7
Classification
Type:
Protein-serine/threonine kinase
Group:
AGC
Family:
GRK
SubFamily:
GRK
Specific Links
Structure
Mol. Mass (Da):
62212
# Amino Acids:
553
# mRNA Isoforms:
1
mRNA Isoforms:
62,212 Da (553 AA; Q8WTQ7)
4D Structure:
NA
1D Structure:
Subfamily Alignment
Domain Distribution:
Kinexus Products
Click on entries below for direct links to relevant products from Kinexus for this protein kinase.
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Post-translation Modifications
For detailed information on phosphorylation of this kinase go to PhosphoNET
Acetylated:
K229, K230, K234, K433.
Serine phosphorylated:
S23-, S36-.
Distribution
Based on gene microarray analysis from the NCBI
Human Tissue Distribution
% Max Expression:
Mean Expression:
Number of Samples:
Standard Deviation:
% Max Expression:
Mean Expression:
Number of Samples:
Standard Deviation:
84
1271
6
754
5
74
6
115
-
-
-
-
2
23
28
70
21
313
10
216
0.5
7
9
4
0.3
4
13
3
8
124
5
178
0.1
2
3
0
14
214
5
322
8
126
5
171
33
503
11
429
9
131
2
10
5
81
5
127
9
142
5
234
3
42
7
68
2
28
9
50
4
58
5
79
29
437
5
597
24
370
28
178
7
114
5
155
0.2
3
3
4
-
-
-
-
15
228
7
243
3
48
5
73
24
370
21
397
3
52
5
76
9
134
5
202
4
66
5
88
-
-
-
-
29
440
12
27
100
1521
13
5305
0.1
2
12
0
45
686
26
596
1.4
21
22
18
Evolution
Species Conservation
PhosphoNET % Identity:
PhosphoNET % Similarity:
Homologene %
Identity:
PhosphoNET % Identity:
PhosphoNET % Similarity:
Homologene %
Identity:
100
100
100
99.5
99.5
99.5
96.9
98
97
-
-
86
-
-
-
85.7
92.8
86
-
-
-
41.9
60.7
-
42.2
60.7
-
-
-
-
48
65.8
-
72.9
84.3
73
68.7
82.8
70
60.2
76
62
-
-
-
38.2
54.3
-
-
-
-
39.4
57.6
-
-
-
-
-
-
-
-
-
-
-
-
-
27.3
45.4
-
22.9
38.1
-
-
-
-
For a wider analysis go to PhosphoNET Evolution in PhosphoNET
Binding Proteins
Examples of known interacting proteins
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| No. | Name – UniProt ID |
|---|---|
| 1 | PDE6D - O43924 |
Regulation
Activation:
NA
Inhibition:
Phosphorylates cone opsins thereby initiating their deactivation.
Synthesis:
NA
Degradation:
NA
Known Upstream Kinases
For further details on these substrates click on the Substrate Short Name or UniProt ID. Phosphosite Location is hyperlinked to PhosphoNET
predictions.
Based on in vitro and/or in vivo phosphorylation data
| Kinase Short Name | UniProt ID (Human) | Phosphosite Location | Phosphosite Sequence | Effect of Phosphorylation |
|---|
Protein Kinase Specificity
Matrix of observed frequency (%) of amino acids in aligned protein substrate phosphosites
Matrix Type:
Predicted from the application of the Kinexus Kinase Substrate Predictor Version 2.0 algorithm, which was trained with over 10,000 kinase-protein substrate pairs and 8,000 kinase-peptide substrate pairs.
Domain #:
1
Inhibitors
For further details on these inhibitors click on the Compound Name and enter it into DrugKiNET or click on the ID's
Based on in vitro and/or in vivo phosphorylation data
| Compound Name | KD, Ki or IC50 (nM) | PubChem ID | ChEMBL ID | PubMed ID |
|---|
Disease Linkage
General Disease Association:
Eye disorders
Specific Diseases (Non-cancerous):
Enhanced S cone syndrome (ESCS)
Comments:
Enhanced S-cone syndrome (ESCS) is an inherited retinal disease characterized by the gain-of-function of photoreceptor cells resulting in increased sensitivity to blue light (mediated by the S-cones). ESCS is inherited in an autosomal recessive manner. Symptoms also include visual loss, night blindness, retinal degeneration, and varying deficits in red and green colour vision. Absence of GRK7 expression from retinal photoreceptor cells has been observed in patients with ESCS, indicating that the absence of GRK7 activity may play a role in the pathogenesis of the disease.
Gene Expression in Cancers:
TranscriptoNET (www.transcriptonet.ca) analysis with mRNA expression data retrieved from the National Center for Biotechnology Information's Gene Expression Omnibus (GEO) database, which was normalized against 60 abundantly and commonly found proteins, indicated altered expression for this protein kinase as shown here as the percent change from normal tissue controls (%CFC) as supported with the Student T-test in human Breast epithelial hyperplastic enlarged lobular units (HELU) (%CFC= -45, p<0.019). The COSMIC website notes an up-regulated expression score for GRK7 in diverse human cancers of 512, which is 1.1-fold of the average score of 462 for the human protein kinases. The down-regulated expression score of 0 for this protein kinase in human cancers was 100% lower than average score of 60 for the human protein kinases.
Mutagenesis Experiments:
Insertional mutagenesis studies in mice have not yet revealed a role for this protein kinase in mouse cancer oncogenesis.
Mutation Rate in All Cancers:
Percent mutation rates per 100 amino acids length in human cancers: 0.1 % in 24917 diverse cancer specimens. This rate is only 38 % higher than the average rate of 0.075 % calculated for human protein kinases in general.
Mutation Rate in Specific Cancers:
Highest percent mutation rates per 100 amino acids length in human cancers: 1.21 % in 15 pituitary cancers tested; 0.61 % in 864 skin cancers tested; 0.5 % in 1270 large intestine cancers tested; 0.21 % in 589 stomach cancers tested; 0.17 % in 1822 lung cancers tested; 0.16 % in 1512 liver cancers tested; 0.15 % in 710 oesophagus cancers tested; 0.15 % in 603 endometrium cancers tested; 0.13 % in 548 urinary tract cancers tested; 0.1 % in 1459 pancreas cancers tested; 0.08 % in 945 upper aerodigestive tract cancers tested.
Frequency of Mutated Sites:
Most frequent mutations with the number of reports indicated in brackets: A154V (4).
Comments:
Only 2 deletions, 1 insertion, and no complex mutations are noted on the COSMIC website.