GRK6

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 dopamin 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).

GRK6 Related Areas

Enzyme>>Protein Kinase>>Intracellular Kinase>>G Protein-Coupled Receptor Kinase (GRK)>>GRK6

Signal Transduction>>Protein Kinase>>Intracellular Kinase>>G Protein-Coupled Receptor Kinase (GRK)>>GRK6

GRK6 Alternative Names

GRK6, FLJ32135, GPRK6 [Homo sapiens]

Grk6, Gprk6 [Mus musculus]

Summaries for GRK6

Entrez Gene summary for GRK6:

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

OMIM - description for GRK6:

By screening a heart cDNA with the catalytic domains of BARK (ADRBK1; 109635), Benovic and Gomez (1993) isolated a cDNA encoding GRK6. The 576-amino acid GRK6 protein is 70% identical to GRK5. PAGE analysis showed expression of a 66-kD protein from an insect cell line.

Wikipedia summary for GRK6:

G protein-coupled receptor kinase 6 is an enzyme that in humans is encoded by the GRK6 gene. 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. GRK6 appears to be involved in responses to morphine

Human GRK6 Protein General Information

 

• Protein names: Recommended name: G protein-coupled receptor kinase 6
• Sequence length: 576 AA.
• Catalytic activity: ATP + [G-protein-coupled receptor] = ADP + [G-protein-coupled receptor] phosphate
• Sequence similarities: Belongs to the protein kinase superfamily. AGC Ser/Thr protein kinase family. GPRK subfamily. Contains 1 AGC-kinase C-terminal domain. Contains 1 protein kinase domain. Contains 1 RGS domain.
• Post-translational modification: It is uncertain whether palmitoylation is on Cys-561 and/or Cys-562 and/or Cys-565.
• Subcellular location: Membrane; Lipid-anchor.
• Tissue specificity: Widely expressed.

General information above from UniProt

Function for GRK6 Protein

UniProtKB:

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 dopamin 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).

Genatlas:

• GRK6 mediates phosphatidylinositol 4,5-biphosphate (PIP2) dependent phosphorylation of beta adrenergic receptor 1
• key regulator of dopaminergic signaling and lymphocyte chemotaxis
• GRK6 is involved in the regulation of oxytocin receptor responsiveness in human myometrial smooth muscle
• GRK6 may play a role in regulating some, but not all morphine-mediated responses
• GRK5/6 is a novel kinases for the single transmembrane receptor LRP6 during Wnt signaling
• GRK6 exhibits lymphoid-restricted expression, and its expression in myeloma cells is regulated via direct association with the heat shock protein 90 (HSP90) chaperone
• potent mechanism for the cytotoxicity of GRK6 inhibition in multiple myeloma (MM) tumor cells

Homology for human GRK6

• ortholog to murine Gprk6