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Tchem
GRK5
G protein-coupled receptor kinase 5

Protein Summary
Description
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
Uniprot Accession IDs
Gene Name
Ensembl ID
  • ENST00000392870
  • ENSP00000376609
  • ENSG00000198873

Symbol
  • GPRK5
  • GPRK5
  • FP2025
Illumination Graph
Knowledge Table
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
ProKinO
Thumbnail image for ProKinO
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.
Target Illumination GWAS Analytics (TIGA)
Thumbnail image for Target Illumination GWAS Analytics (TIGA)
TIGA scores and ranks GWAS discovered associations according to the quantity and quality of the evidence supporting the association.
GENEVA
Thumbnail image for GENEVA
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
Thumbnail image for GlyGen
GlyGen is a data integration and dissemination project for carbohydrate and glycoconjugate related data.
IDG Development Level Summary
Tdark

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)
Tbio

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
Tchem

Target has at least one ChEMBL compound with an activity cutoff of < 30 nM - AND - satisfies the preceding conditions

Active Ligands: 2
Tclin

Target has at least one approved drug - AND - satisfies the preceding conditions

Active Drug: 0
GWAS Traits (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
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)
RepresentationColor Scheme

Click on a row in the table to change the structure displayed.
More information can be found at RCSB PDB

AF-P34947-F1-model_v1

AlphaFold Structures Developed by DeepMind and EMBL-EBI

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)
G alpha (q) signalling events (R-HSA-416476)

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)
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
Tchem
Family:  Kinase
Novelty:  0.02740874
p_int:  1
Score:  0.939
Data Source:  BioPlex,STRINGDB
ARRB1
Tbio
Novelty:  0.00262758
Score:  0.989
Data Source:  STRINGDB
AGTR1
Tclin
Family:  GPCR
Novelty:  0.00033439
Score:  0.979
Data Source:  STRINGDB
ADRB2
Tclin
Family:  GPCR
Novelty:  0.00041821
Score:  0.975
Data Source:  Reactome,STRINGDB
ARRB2
Tbio
Novelty:  0.00148149
Score:  0.968
Data Source:  STRINGDB
SNCA
Tchem
Novelty:  0.00012042
Score:  0.964
Data Source:  STRINGDB
TRHR
Tclin
Family:  GPCR
Novelty:  0.01143992
Score:  0.961
Data Source:  STRINGDB
NTSR1
Tchem
Family:  GPCR
Novelty:  0.00067612
Score:  0.957
Data Source:  STRINGDB
LRP6
Tbio
Novelty:  0.00305615
Score:  0.951
Data Source:  STRINGDB
GNRHR
Tclin
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
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