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Tchem
GRK6
G protein-coupled receptor kinase 6

Protein Summary
Description
Specifically phosphorylates the activated forms of G protein-coupled receptors. Such receptor phosphorylation initiates beta-arrestin-mediated receptor desensitization, internalization, and signaling events leading to their desensitization. Seems to be involved in the desensitization of D2-like dopamine receptors in striatum and chemokine receptor CXCR4 which is critical for CXCL12-induced cell chemotaxis (By similarity). Phosphorylates rhodopsin (RHO) (in vitro) and a non G-protein-coupled receptor: LRP6 during Wnt signaling (in vitro). 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 their deactivation. Several transcript variants encoding different isoforms have been described for this gene. [provided by RefSeq, Jul 2008]
Uniprot Accession IDs
Gene Name
Ensembl ID
  • ENST00000355472
  • ENSP00000347655
  • ENSG00000198055
  • ENST00000355958
  • ENSP00000348230
  • ENST00000528793
  • ENSP00000433511

Symbol
  • GPRK6
  • GPRK6
Illumination Graph
Knowledge Table
Most Knowledge About
Knowledge Value (0 to 1 scale)
protein domain
0.97
transcription factor perturbation
0.97
molecular function
0.94
transcription factor
0.87
transcription factor binding site profile
0.81


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: 52.67   (req: < 5)
Gene RIFs: 31   (req: <= 3)
Antibodies: 359   (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: 52.67   (req: >= 5)
Gene RIFs: 31   (req: > 3)
Antibodies: 359   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 6
Tchem

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

Active Ligands: 13
Tclin

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

Active Drug: 0