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

• P43250
• O60541
• Q13652

Gene Name

• GRK6

Ensembl ID

• ENST00000355472
• ENSP00000347655
• ENSG00000198055
• ENST00000355958
• ENSP00000348230
• ENST00000528793
• ENSP00000433511

Symbol

• GPRK6
• GPRK6

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

Protein Classes

PANTHER Classes

Protein / Transferase / Kinase / Protein Kinase / Non-receptor Serine/threonine Protein Kinase / G Protein-coupled Receptor Kinase 6

DTO Classes

Protein / Kinase / Protein Kinase / Agc Group / Grk Family / Grk Subfamily / G Protein-coupled Receptor Kinase 6

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