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Tchem
GRK4
G protein-coupled receptor kinase 4

Protein Summary
Description
Specifically phosphorylates the activated forms of G protein-coupled receptors. GRK4-alpha can phosphorylate rhodopsin and its activity is inhibited by calmodulin; the other three isoforms do not phosphorylate rhodopsin and do not interact with calmodulin. GRK4-alpha and GRK4-gamma phosphorylate DRD3. Phosphorylates ADRB2. This gene encodes a member of the guanine nucleotide-binding protein (G protein)-coupled receptor kinase subfamily of the Ser/Thr protein kinase family. The protein phosphorylates the activated forms of G protein-coupled receptors thus initiating its deactivation. This gene has been linked to both genetic and acquired hypertension. Several transcript variants encoding different isoforms have been found for this gene. [provided by RefSeq, Nov 2013]
Uniprot Accession IDs
Gene Name
Ensembl ID
  • ENST00000345167
  • ENSP00000264764
  • ENSG00000125388
  • ENST00000398051
  • ENSP00000381128
  • ENST00000398052
  • ENSP00000381129
  • ENST00000504933
  • ENSP00000427445

Symbol
  • GPRK2L
  • GPRK4
  • IT11
  • GPRK4
  • GRK4a
  • GPRK2L
Illumination Graph
Knowledge Table
Most Knowledge About
Knowledge Value (0 to 1 scale)
protein domain
0.97
molecular function
0.93
histone modification site profile
0.88
transcription factor binding site profile
0.87
tissue
0.64


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: 83.23   (req: < 5)
Gene RIFs: 46   (req: <= 3)
Antibodies: 243   (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: 83.23   (req: >= 5)
Gene RIFs: 46   (req: > 3)
Antibodies: 243   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 8
Tchem

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

Active Ligands: 3
Tclin

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

Active Drug: 1