GRK5
G protein-coupled receptor kinase 5
Protein Classes
Protein Summary
Serine/threonine kinase that phosphorylates preferentially the activated forms of a variety of G-protein-coupled receptors (GPCRs). Such receptor phosphorylation initiates beta-arrestin-mediated receptor desensitization, internalization, and signaling events leading to their down-regulation. Phosphorylates a variety of GPCRs, including adrenergic receptors, muscarinic acetylcholine receptors (more specifically Gi-coupled M2/M4 subtypes), dopamine receptors and opioid receptors. In addition to GPCRs, also phosphorylates various substrates: Hsc70-interacting protein/ST13, TP53/p53, HDAC5, and arrestin-1/ARRB1. Phosphorylation of ARRB1 by GRK5 inhibits G-protein independent MAPK1/MAPK3 signaling downstream of 5HT4-receptors. Phosphorylation of HDAC5, a repressor of myocyte enhancer factor 2 (MEF2) leading to nuclear export of HDAC5 and allowing MEF2-mediated transcription. Phosphorylation of TP53/p53, a crucial tumor suppressor, inhibits TP53/p53-mediated apoptosis. Phosphorylation of ST1 ...more
- ENST00000392870
- ENSP00000376609
- ENSG00000198873
- GPRK5
- GPRK5
- FP2025
Most Knowledge About | Knowledge Value
(0 to 1 scale) | ||
|---|---|---|---|
molecular function | 0.98 | ||
disease perturbation | 0.95 | ||
protein domain | 0.92 | ||
transcription factor binding site profile | 0.86 | ||
chemical bioactivity profile | 0.71 | ||
Related Tools
The ProKinO is a protein kinase-specific ontology, which provides a controlled vocabulary of terms, their hierarchy, and relationships unifying sequence, structure, function, mutation and pathway information on kinases.
TIGA scores and ranks GWAS discovered associations according to the quantity and quality of the evidence supporting the association.
GENEVA (GENe Expression Variance Analysis) allows you to identify RNA-sequencing datasets from the Gene Expression Omnibus (GEO) that contain conditions modulating a gene or a gene signature.
GlyGen is a data integration and dissemination project for carbohydrate and glycoconjugate related data.
IDG Development Level Summary
These are targets about which virtually nothing is known. They do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:
Pubmed score: 113.71 (req: < 5)
Gene RIFs: 60 (req: <= 3)
Antibodies: 473 (req: <= 50)
These targets do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:
Pubmed score: 113.71 (req: >= 5)
Gene RIFs: 60 (req: > 3)
Antibodies: 473 (req: > 50)
- OR - satisfy the following criterion:
Gene Ontology Terms: 17
Target has at least one ChEMBL compound with an activity cutoff of < 30 nM - AND - satisfies the preceding conditions
Active Ligands: 2
Target has at least one approved drug - AND - satisfies the preceding conditions
Active Drug: 0
Active Ligands (2)
1 – 2 of 2
GWAS Traits (14)
Items per page:
1 – 5 of 14
GWAS Trait | EFO ID | Study Count | SNP Count | Beta Count | Odds Ratio | Evidence (Mean Rank Score) | Provenance | ||
|---|---|---|---|---|---|---|---|---|---|
CCL17 measurement | 1 | 1 | 1 | 86.5 | |||||
mean platelet volume | 3 | 1 | 3 | 85.4 | |||||
platelet aggregation | 1 | 1 | 1 | 82.8 | |||||
venous thromboembolism | 3 | 1 | 1 | 1.1 | 70.2 | ||||
lymphocyte count | 2 | 1 | 2 | 66 | |||||
Items per page:
1 – 5 of 14
GWAS Trait | EFO ID | Beta Count | Odds Ratio | Evidence (Mean Rank Score) | Provenance | ||
|---|---|---|---|---|---|---|---|
CCL17 measurement | 1 | 86.5 | |||||
mean platelet volume | 3 | 85.4 | |||||
platelet aggregation | 1 | 82.8 | |||||
venous thromboembolism | 1 | 1.1 | 70.2 | ||||
lymphocyte count | 2 | 66 | |||||
Orthologs (12)
1 – 5 of 12
Species | Name | Source ID | Gene ID | OMA | EggNOG | Inparanoid | ||
|---|---|---|---|---|---|---|---|---|
Chimp | G protein-coupled receptor kinase 5 | VGNC:4700 | 466217 | |||||
Macaque | G protein-coupled receptor kinase 5 | 100427251 | ||||||
Mouse | MGI:109161 | 14773 | ||||||
Rat | RGD:61985 | 59075 | ||||||
Dog | G protein-coupled receptor kinase 5 | VGNC:41505 | 486915 | |||||
Species | Name | OMA | EggNOG | Inparanoid | ||
|---|---|---|---|---|---|---|
Chimp | G protein-coupled receptor kinase 5 | |||||
Macaque | G protein-coupled receptor kinase 5 | |||||
Mouse | ||||||
Rat | ||||||
Dog | G protein-coupled receptor kinase 5 | |||||
Protein Structure (2 Structures, 1 AlphaFold Model)
Click on a row in the table to change the structure displayed.
More information can be found at RCSB PDB
1 – 2 of 2
PDB Structure Id | Ligand | Method | Resolution (Å) | Residues | Fraction of Total Protein | Pub Year | Title |
|---|
PDB Structure Id | Fraction of Total Protein | Resolution | Pub Year |
|---|
Pathways (21)
Reactome (5)
KEGG (3)
PathwayCommons (10)
WikiPathways (3)
Click on a row in the table to change the structure displayed.
Items per page:
1 – 5 of 5
Data Source | Name | Explore in Pharos | Explore in Source | ||
|---|---|---|---|---|---|
Reactome | G alpha (q) signalling events | ||||
Reactome | G alpha (s) signalling events | ||||
Reactome | GPCR downstream signalling | ||||
Reactome | Signal Transduction | ||||
Reactome | Signaling by GPCR | ||||
Name | Explore in Pharos | Explore in Source | ||
|---|---|---|---|---|
G alpha (q) signalling events | ||||
G alpha (s) signalling events | ||||
GPCR downstream signalling | ||||
Signal Transduction | ||||
Signaling by GPCR | ||||
Gene Ontology Terms (22)
Functions (6)
Components (5)
Processes (11)
Items per page:
10
1 – 6 of 6
GO Term | Evidence | Assigned by | ||
|---|---|---|---|---|
Inferred from Direct Assay (IDA) | UniProtKB | |||
Inferred from Mutant Phenotype (IMP) | CACAO | |||
Traceable Author Statement (TAS) | ProtInc | |||
Traceable Author Statement (TAS) | ProtInc | |||
Inferred from Electronic Annotation (IEA) | UniProtKB-KW | |||
Inferred from Electronic Annotation (IEA) | UniProtKB-EC | |||
Protein-Protein Interactions (223)
1 – 10 of 223
GRK6
Family: Kinase
Novelty: 0.02740874
p_int: 1
Score: 0.939
Data Source: BioPlex,STRINGDB
ARRB1
Novelty: 0.00262758
Score: 0.989
Data Source: STRINGDB
AGTR1
Family: GPCR
Novelty: 0.00033439
Score: 0.979
Data Source: STRINGDB
ADRB2
Family: GPCR
Novelty: 0.00041821
Score: 0.975
Data Source: Reactome,STRINGDB
ARRB2
Novelty: 0.00148149
Score: 0.968
Data Source: STRINGDB
SNCA
Novelty: 0.00012042
Score: 0.964
Data Source: STRINGDB
TRHR
Family: GPCR
Novelty: 0.01143992
Score: 0.961
Data Source: STRINGDB
NTSR1
Family: GPCR
Novelty: 0.00067612
Score: 0.957
Data Source: STRINGDB
LRP6
Novelty: 0.00305615
Score: 0.951
Data Source: STRINGDB
GNRHR
Family: GPCR
Novelty: 0.00203671
Score: 0.949
Data Source: STRINGDB
Publication Statistics
PubMed Score 113.71
PubMed score by year
PubTator Score 123.63
PubTator score by year
Patents
Amino Acid Sequence
Residue Counts
Protein Sequence
ProtVista Viewer
Ortholog Sequence Conservation
PolarG S T Y C
NeutralQ N
BasicK R H
AcidicD E
HydrophobicA V L I P W F M
Find similar targets by:
UniProt Keyword
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GWAS Trait
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