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

• P32298
• O00641
• O00642
• Q13293
• Q13294
• Q13295
• Q14453
• Q14725
• Q15313
• Q15314
• Q15315
• Q15316
• Q17RH6
• Q53EQ8

Gene Name

• GRK4

Ensembl ID

• ENST00000345167
• ENSP00000264764
• ENSG00000125388
• ENST00000398051
• ENSP00000381128
• ENST00000398052
• ENSP00000381129
• ENST00000504933
• ENSP00000427445

Symbol

• GPRK2L
• GPRK4
• IT11
• GPRK4
• GRK4a
• GPRK2L

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

Protein Classes

PANTHER Classes

Protein / Transferase / Kinase / Protein Kinase / Non-receptor Serine/threonine Protein Kinase / G Protein-coupled Receptor Kinase 4

DTO Classes

Protein / Kinase / Protein Kinase / Agc Group / Grk Family / Grk Subfamily / G Protein-coupled Receptor Kinase 4

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