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FLASH GENE
Symbol GRK4 contributors: mct/npt - updated : 10-11-2014
HGNC name G protein-coupled receptor kinase 4
HGNC id 4543
PROTEIN
PHYSICAL PROPERTIES
STRUCTURE
motifs/domains
  • a RGS domain
  • a protein kinase domain
  • HOMOLOGY
    interspecies homolog to Drosophila G protein coupled receptor kinase 2
    ortholog to murine Gprk2l
    Homologene
    FAMILY
  • G protein coupled receptor family
  • Ser/Thr family of protein kinases
  • GPRK subfamily
  • CATEGORY enzyme , receptor
    SUBCELLULAR LOCALIZATION     intracellular
    intracellular,cytoplasm,cytosolic
    text
  • associate with the cell membrane through palmitoylation of the cysteine residue at its C terminus
  • both DRD3 and GRK4 co-localize in lipid rafts of human renal proximal tubule cells (Villar 2009)
  • basic FUNCTION
  • inhibiting the dopamine receptor D1 (DRD1) from increasing sodium excretion
  • mediating the pressure and natriuresis relation
  • involved in renal sodium handling and blood pressure regulation (Hasenkamp 2008)
  • required for DRD3-mediated mitogenesis and activation of the MAP kinase pathway inrenal proximal tubule cells (Villar 2009)
  • via regulation of arterial AGTR1 expression and function, participates in the pathogenesis of conduit vessel abnormalities in hypertension
  • CELLULAR PROCESS
    PHYSIOLOGICAL PROCESS
    PATHWAY
    metabolism
    signaling signal transduction
    a component
    INTERACTION
    DNA
    RNA
    small molecule
    protein
  • interaction between DRD3 and GRK4 (Villar 2009)
  • cell & other
    REGULATION
    ASSOCIATED DISORDERS
    corresponding disease(s)
    Susceptibility to essential hypertension
    Variant & Polymorphism other
  • variant in isoform GRK4 gamma associated with essential hypertension
  • 65L allele is associated with stress-induced urinary sodium excretion reduction, suggesting impaired sodium handling in black normotensive adolescents
  • Candidate gene
    Marker
    Therapy target
    ANIMAL & CELL MODELS