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GRK2 / ADRBK1  Protein

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Expression host: Baculovirus-Insect Cells  
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    GRK2 / ADRBK1 Summary & Protein Information

    GRK2 / ADRBK1 Background

    Gene Summary: The product of this ADRBK1 gene phosphorylates the beta-2-adrenergic receptor and appears to mediate agonist-specific desensitization observed at high agonist concentrations. GRK2 is an ubiquitous cytosolic enzyme that specifically phosphorylates the activated form of the beta-adrenergic and related G-protein-coupled receptors. Abnormal coupling of beta-adrenergic receptor to G protein is involved in the pathogenesis of the failing heart. [provided by RefSeq, Jul 2008]
    General information above from NCBI
    Catalytic activity: ATP + [beta-adrenergic receptor] = ADP + [beta-adrenergic receptor] phosphate.
    Enzyme regulation: ENZYME REGULATION: In contrast to other AGC family kinases, the catalytic activity is solely regulated by the binding of substrates and ligands, not by phosphorylation of the kinase domain. {ECO:0000250|UniProtKB:P21146}.
    Subunit structure: Interacts with GIT1 (By similarity). Interacts with, and phosphorylates chemokine-stimulated CCR5. Interacts with ARRB1. Interacts with LPAR1 and LPAR2. Interacts with RALA in response to LPAR1 activation. ADRBK1 and RALA mutually inhibit each other's binding to LPAR1. {ECO:0000250, ECO:0000269|PubMed:10085131, ECO:0000269|PubMed:19306925, ECO:0000269|PubMed:9501202}.
    Domain: The PH domain binds anionic phospholipids and helps recruiting ADRBK1 from the cytoplasm to plasma membrane close to activated receptors. It mediates binding to G protein beta and gamma subunits, competing with G-apha subunits and other G-betagamma effectors. {ECO:0000250|UniProtKB:P21146}.
    Subcellular location: Cytoplasm {ECO:0000250|UniProtKB:P21146}. Cell membrane {ECO:0000250|UniProtKB:P21146}.
    Tissue specificity: Expressed in peripheral blood leukocytes. {ECO:0000269|PubMed:10085131}.
    Sequence similarity: Belongs to the protein kinase superfamily. AGC Ser/Thr protein kinase family. GPRK subfamily. {ECO:0000305}.; Contains 1 AGC-kinase C-terminal domain. {ECO:0000305}.; Contains 1 PH domain. {ECO:0000255|PROSITE-ProRule:PRU00145}.; Contains 1 protein kinase domain. {ECO:0000255|PROSITE-ProRule:PRU00159}.; Contains 1 RGS domain. {ECO:0000255|PROSITE-ProRule:PRU00171}.
    General information above from UniProt

    G-protein coupled receptor kinase 2 (GRK2), also referred as Adrenergic, beta, receptor kinase 1 (ADRBK1), is a ubiquitous member of the G protein-coupled receptor kinase (GRK) family that appears to play a central, integrative role in signal transduction cascades. GRK2 can phosphorylate a growing number of non-GPCR substrates and associate with a variety of proteins related to signal transduction, thus suggesting that this kinase could also have diverse 'effector' functions. GRK2 has been reported to interact with a variety of signal transduction proteins related to cell migration such as MEK, Akt, PI3Kgamma or GIT. Interestingly, the levels of expression and activity of this kinase are altered in a number of inflammatory disorders (as rheumatoid arthritis or multiple sclerosis), thus suggesting that GRK2 may play an important role in the onset or development of these pathologies. The important physiological function of GRK2 as a modulator of the efficacy of GPCR signal transduction systems is exemplified by its relevance in cardiovascular physiopathology as well as by its emerging role in the regulation of chemokine receptors. Besides its canonical role in the modulation of the signalling mediated by many G protein-coupled receptors (GPCR), this protein can display a very complex network of functional interactions with a variety of signal transduction partners, in a stimulus, cell type, or context-specific way.

    GRK2 / ADRBK1 Alternative Name

    GRK2,BARK1,BETA-ARK1, [homo-sapiens]
    BETA-ARK1,FLJ16718,ADRBK1,BARK1,GRK2, [human]
    Bark-1,Adrbk1,Adrbk-1,betaARK1,GRK2, [mouse]
    GRK2,Bark-1,Adrbk-1,betaARK,betaARK1, [mus-musculus]

    GRK2 / ADRBK1 Related Studies

  • Penela P, et al. (2010) The complex G protein-coupled receptor kinase 2 (GRK2) interactome unveils new physiopathological targets. Br J Pharmacol. 160(4): 821-32.
  • Penela P, et al. (2008) G protein-coupled receptor kinase 2 (GRK2) in migration and inflammation. Arch Physiol Biochem. 114(3): 195-200.
  • Aragay AM, et al. (1998) protein-coupled receptor kinase 2 (GRK2): mechanisms of regulation and physiological functions. FEBS Lett. 430(1-2): 37-40.