GRK5
G protein-coupled receptor kinase 5
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 | ||
Protein Classes
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
Protein Sequence and Structure
Residue Counts
Protein Sequence
ProtVista Viewer
Expression Data (0 Tissues)
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.
ARCHS4 provides access to gene-function predictions based on RNA-seq co-expression, and gene expression levels across cell and tissues.
Approved Drugs (0)
Active Ligands (2)
Protein-Protein Interactions (223)
Nearest Tclin Targets (4)
Downstream (4)
1 – 4 of 4
Pathways (21)
Reactome (5)
KEGG (3)
PathwayCommons (10)
WikiPathways (3)
Click on a row in the table to change the structure displayed.
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 | ||||
Viral Interactions (0)
Gene Ontology Terms (22)
Functions (6)
Components (5)
Processes (11)
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 | |||
Disease Associations ()
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 | |||||
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 | |||||
1 | 1.1 | 70.2 | |||||
lymphocyte count | 2 | 66 | |||||
Find similar targets by:
IDG Resources
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 | |||||
Publication Statistics
PubMed Score 113.71
PubMed score by year
PubTator Score 123.63
PubTator score by year
Patents
Patents by year
Related Publications
Text Mined References (92)
GeneRif Annotations (60)
Items per page:
0 of 0
PMID | Year | Title |
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