Human Beta-adrenergic receptor kinase 1(ADRBK1) ELISA kit

Code CSB-EL001394HU
Size 96T,5×96T,10×96T
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Product Details

Target Name adrenergic, beta, receptor kinase 1
Alternative Names ADRBK1 ELISA Kit; Adrenergic beta receptor kinase 1 ELISA Kit; ARBK1_HUMAN ELISA Kit; BARK ELISA Kit; BARK1 ELISA Kit; Beta adrenergic receptor kinase 1 ELISA Kit; Beta ARK 1 ELISA Kit; Beta ARK1 ELISA Kit; Beta-adrenergic receptor kinase 1 ELISA Kit; Beta-ARK-1 ELISA Kit; FLJ16718 ELISA Kit; G protein coupled receptor kinase 2 ELISA Kit; G-protein coupled receptor kinase 2 ELISA Kit; GRK2 ELISA Kit
Abbreviation ADRBK1
Uniprot No. P25098
Species Homo sapiens (Human)
Sample Types serum, plasma, tissue homogenates, cell lysates
Detection Range 18.75 pg/mL-1200 pg/mL
Sensitivity 4.68 pg/mL
Assay Time 1-5h
Sample Volume 50-100ul
Detection Wavelength 450 nm
Research Area Signal Transduction
Assay Principle quantitative
Measurement Sandwich
Intra-assay Precision (Precision within an assay): CV%<8%      
Three samples of known concentration were tested twenty times on one plate to assess.  
Inter-assay Precision (Precision between assays): CV%<10%      
Three samples of known concentration were tested in twenty assays to assess.    
To assess the linearity of the assay, samples were spiked with high concentrations of human ADRBK1 in various matrices and diluted with the Sample Diluent to produce samples with values within the dynamic range of the assay.
  Sample Serum(n=4)  
1:1 Average % 91  
Range % 88-94  
1:2 Average % 95  
Range % 90-101  
1:4 Average % 97  
Range % 94-102  
1:8 Average % 94  
Range % 91-99  
The recovery of human ADRBK1 spiked to levels throughout the range of the assay in various matrices was evaluated. Samples were diluted prior to assay as directed in the Sample Preparation section.
Sample Type Average % Recovery Range  
Serum (n=5) 90 87-93  
EDTA plasma (n=4) 99 93-104  
Typical Data
These standard curves are provided for demonstration only. A standard curve should be generated for each set of samples assayed.
pg/ml OD1 OD2 Average Corrected  
1200 2.036 2.166 2.101 1.927  
600 1.373 1.405 1.389 1.215  
300 0.997 0.957 0.977 0.803  
150 0.633 0.675 0.654 0.480  
75 0.392 0.402 0.397 0.223  
37.5 0.294 0.284 0.289 0.115  
18.75 0.241 0.233 0.237 0.063  
0 0.167 0.180 0.174    
and FAQs
Storage Store at 2-8°C. Please refer to protocol.
Lead Time 7-14 working days

Target Data

Function Specifically phosphorylates the agonist-occupied form of the beta-adrenergic and closely related receptors, probably inducing a desensitization of them. Key regulator of LPAR1 signaling. Competes with RALA for binding to LPAR1 thus affecting the signaling properties of the receptor. Desensitizes LPAR1 and LPAR2 in a phosphorylation-independent manner.
Gene References into Functions
  1. M3R activation-induced GRK2 recruitment is Ggamma subtype dependent in which Gbetagamma dimers with low cell membrane-affinity Ggamma9 exhibited a two-fold higher GRK2-recruitment compared to high affinity Ggamma3 expressing cells. PMID: 29864421
  2. Chronic/pathologic GPCR signaling elicits the interaction of the G-protein Gbetagamma subunit with GPCR kinase 2 (GRK2), targeting the receptor for internalization, scaffolding to pathologic signals, and receptor degradation. Targeting this pathologic Gbetagamma-GRK2 interaction has been suggested as a possible strategy for the treatment of HF. PMID: 28130200
  3. A novel regulatory role of GRK2 was proposed for the ubiquitination of beta-arrestin in the context of the PKC-mediated heterologous regulation of GPCRs. PMID: 29054428
  4. eIF3d promotes gallbladder cancer (GBC) progression mainly via eIF3d-GRK2-AKT axis and it may be used as a prognostic factor. The therapeutic targeting of eIF3d-GRK2 axis may be a potential treatment approach for GBC. PMID: 28594409
  5. KHSV miR-K3 activates the GRK2/CXCR2/AKT axis inducing KSHV-induced angiogenesis and promoting KSHV latency. PMID: 27058419
  6. Compared to the original peptide, a modified peptide (Ac-EEMEFSEAEANMN-NH2) exhibited markedly higher affinity for GRK2, but very low affinity for GRK5, suggesting that it can be a sensitive and selective peptide for GRK2 PMID: 27714516
  7. Low grk2 expression is associated with lung metastasis in gastric cancer. PMID: 28843497
  8. Lowering the level of cellular FLNA caused an elevation in RalA activity and resulted in selective interference with the normal intracellular trafficking and signaling of D2R through GRK2. PMID: 27188791
  9. Results demonstrate that GPR3 signals at the plasma membrane and can be silenced by GRK2/beta-arrestin overexpression. These results also strongly implicate the serine and/or threonine residues in the third intracellular loop in the regulation of GPR3 activity. PMID: 23826079
  10. GRK2 is negatively related to IGF1R and IGF1R, but not GRK2, was associated with the tumour-node-metastasis stage and overall and disease-free survival in hepatocellular carcinoma. PMID: 28202495
  11. The tyrosine-phosphorylated GRK2 mediates this inhibition by acting on the second intracellular loop of D3R. PMID: 28579429
  12. GRK2 is overexpressed in pancreatic cancer, and might serve as a potential indicator of unfavorable prognosis. PMID: 27346572
  13. Data, including data from studies in heterozygous knockout mice, suggest that GRK2 is involved in TNFalpha-induced wound healing in epithelial cells of the colon; GRK2 appears to inhibit TNFalpha-induced apoptosis; GRK2 inhibits TNFalpha-induced ERK activation by inhibiting generation of reactive oxygen species. Homozygous knockout of GRK2 is embryonically lethal in mice. PMID: 28572156
  14. The dominant model (CC vs. CT+TT) of rs1894111 polymorphism in the ADRBK1 gene might be associated with low-renin hypertension in Han Chinese. PMID: 27555048
  15. Our data suggest that GRK2 acts as an important onco-modulator by strengthening the functionality of key players in breast tumorigenesis such as HDAC6 and Pin1. PMID: 27720394
  16. GRK2 may inhibit IGF1-induced human hepatocellular carcinoma cell growth and migration through downregulation of EGR1. PMID: 26936374
  17. It is a critical factor in diabetic endothelial dysfunction and plays a role in many physiological functions including regulation of G-protein-coupled receptors (GPCRs). (review) PMID: 26234354
  18. Suggest role for GRK2 in the regulating cardiac hypertrophy. PMID: 26224342
  19. the dual-specific GRK2 and ERK cascade inhibitor, RKIP (Raf kinase inhibitor protein), triggered dysfunctional cardiomyocyte energetics and the expression of heart failure-promoting Pparg-regulated genes. PMID: 26670611
  20. Acute mental stress significantly increased GRK2 density in in peripheral blood mononuclear cells of young adult males. PMID: 26706289
  21. It plays a role in progression of Vasculature which is affected by insulin resistance and type 2 diabetes expresses high levels of GRK2 PMID: 26447102
  22. Data suggest that, by targeting/repressing GRK2, microRNA-K3 of Kaposi sarcoma-associated herpesvirus (KSHV) facilitates migration and invasion of vascular endothelial cells via activation of CXCR2/AKT signaling. PMID: 26402907
  23. Acute aerobic exercise induces a greater GRK2 expression in women than men, while increased cardiorespiratory fitness is associated with exercise-induced GRK2 expression in PBMCs PMID: 26092485
  24. G protein beta subunits (Gb) bind to DDB1 and Gb2 targets GRK2 for ubiquitylation by the DDB1-CUL4A-ROC1 ubiquitin ligase. PMID: 25982117
  25. A thorough understanding of the functions of GRK2 in the heart is necessary in order to finalize it as a candidate for drug development. PMID: 24702056
  26. Knockdown of ADRBK1 gene has detrimental effects on breast cancer cell growth. PMID: 25279970
  27. Results uncovered that Gaq binding to GRK2 enhances the recruitment of GRK2 to M3-ACh receptors. PMID: 25316767
  28. These data demonstrate that GRK2 modulates FcinRI signaling in mast cells via at least two mechanisms.One involves GRK2-RH and modulates tyrosine phosphorylation of Syk, and the other is mediated via the phosphorylation of p38 and Akt. PMID: 24904059
  29. Data indicate that residues on the G-protein coupled receptor kinase 2 (GRK2) N terminus and kinase domain extension collaborate to create a G protein-coupled receptor (GPCR) docking site. PMID: 25049229
  30. Low levels of GRK2/GRK5 causes a slow and not complete desensitization/down-regulation of GPR17. PMID: 24613411
  31. GRK2 is localized to centrosomes and plays a central role in mitogen-promoted centrosome separation. PMID: 23904266
  32. The gene expression levels of TREM1 in PMNs isolated from patients with bacterial infections may be used as a surrogate biomarker for determining the severity. PMID: 24465168
  33. Changes in lymphocyte GRK2 after exercise training can strongly predict outcome in advanced heart failure. PMID: 23689525
  34. This review discusses recently discovered roles of GRK2 as a biomarker in cardiomyocyte metabolism and myocardial contraction. PMID: 24812353
  35. decreased endothelial Grk2 dosage accelerated tumor growth, along with reduced pericyte vessel coverage and enhanced macrophage infiltration, and this transformed environment promoted decreased GRK2 in breast cancer vessels PMID: 24135140
  36. This study showed that, among GRK2, beta-arrestin 1, and beta-arretin 2, beta-arrestin 1 and GRK2 seem to have a role in modulating GH secretion during somatostatin analog treatment. PMID: 24169548
  37. Desensitization and internalization of endothelin receptor A: impact of G protein-coupled receptor kinase 2 (GRK2)-mediated phosphorylation. PMID: 24064210
  38. Data indicate that CXCL12-induced phosphorylation at CXCR4 S346/347 was mediated by GRK2/3. PMID: 23734232
  39. GRK2 takes part in the regulation of the initial inflammatory response during mycobacterial infection. PMID: 23312955
  40. We further detected that reduced level of GRK2 induced a small cell cycle arrest at G2/M phase by enhancing the expression of cyclin A, B1, and E PMID: 23460259
  41. Data suggest that specific serine/threonine residues in DRD2 (dopamine receptor D2) are involved in regulation of DRD2 endocytosis by GRK2 and GASP1 (G protein-coupled receptor associated sorting protein 1). PMID: 23082996
  42. Gene transfer of human GRK2 inhibitory peptide preserved regional/global systolic function after acute MI without arresting progressive ventricular remodeling. PMID: 23208013
  43. This study identify that GRK2 as a potential molecular link between inflammation and mGluR-mediated sensitization. PMID: 23494575
  44. this study provides evidence that GRK2 mediates phosphorylation-independent mGluR5 desensitization via the interaction between the RGS domain and Galphaq in HEK 293 cells. PMID: 23705503
  45. Increased localization is seen in heart mitochondria from cardiac-specific GRK2 transgenic mice compared with normal littermate controls. PMID: 23467820
  46. GRK2 dynamically associates with and phosphorylates HDAC6 to stimulate its alpha-tubulin deacetylase activity at specific cellular localizations such as the leading edge of migrating cells, thus promoting local tubulin deacetylation and enhanced motility. PMID: 23076141
  47. Persistent hyperalgesia in GRK2-deficient mice is associated with an increase in spinal cord microglia/macrophages. PMID: 22731384
  48. Inhibition of G-protein-coupled receptor kinase 2 (GRK2) triggers the growth-promoting mitogen-activated protein kinase (MAPK) pathway PMID: 23362259
  49. a novel role for IL-8 in inhibiting betaAR agonist-stimulated alveolar epithelial fluid transport via GRK2/PI3K-dependent mechanisms. PMID: 23221335
  50. These data suggest cell type- and subcellular compartment-dependent differences in GRK/arrestin-mediated desensitization and signaling. PMID: 23139825
  51. Elevation of lymphocyte GRK2 levels in chronic heart failure is associated with heart ejection fraction. PMID: 20684281
  52. The authors found that GRK2 participates in multiple distinct steps of the flavivirus life cycle by promoting both entry and RNA synthesis. PMID: 23029581
  53. GRK2 exerts a strong negative effect on beta-arrestin-dependent signaling through its competition with GRK5 and GRK6 for receptor phosphorylation PMID: 22735336
  54. GRK2-HDAC6 functional interaction may have important implications in pathological contexts related to epithelial cell migration PMID: 22589388
  55. These data show that NPFF-induced heterologous desensitization of MOP receptor signaling is mediated by GRK2 and could involve transphosphorylation within the heteromeric receptor complex. PMID: 22375000
  56. in preeclamptic or gestational hypertensive women, elevated GRK2 levels in the umbilical vasculature is correlated to elevated blood pressure levels, with a likely compensatory rather than causative role PMID: 22089113
  57. A reduced cortical concentration of GRK2 in schizophrenia (resembling that in aging) may result in altered G protein-dependent signaling, thus contributing to prefrontal deficits in schizophrenia. PMID: 21784156
  58. Increased GRK2 correlates with clinical severity using the INTERMACS scale and LV stroke volume, supporting it as a potential target in advanced heart failure. PMID: 22196842
  59. find that a balanced, GRK2/HDAC6-mediated regulation of tubulin acetylation differentially modulates the early and late stages of cellular spreading PMID: 22193721
  60. The data show a novel sub-cellular localization of GRK2 in the mitochondria and an unexpected role in regulating mitochondrial biogenesis and ATP generation. PMID: 21983013
  61. betaarr2 competes with GRK2 for interaction with the activated and GRK phosphorylated GLP-1R, suggesting a new role of betaarr2 in regulating the orchestration of GRK2 functionality PMID: 21952200
  62. GRK2 is a key regulator of the transition from acute to chronic inflammatory pain. Review. PMID: 21473908
  63. GRK2 induces desensitization of H2R through a phosphorylation-independent and RGS-dependent mechanism PMID: 21705320
  64. Metoprolol can inhibit the expression of GRK2 in lymphocyte of advanced elderly patients with chronic heart failure. PMID: 20501412
  65. Increased GRK2 gene expression may play an important role in cardiac dysfunction in diabetes. PMID: 20335112
  66. elevated levels of MIF are associated with cardiac dysfunction in diabetic patients, and the MIF effects are mediated by GRK2 PMID: 21283592
  67. Regulation of the epithelial Na+ channel by the RH domain of G protein-coupled receptor kinase, GRK2, and Galphaq/11. PMID: 21464134
  68. An ADRBK1 SNP (rs1894111 G>A) showed a signal for association with systolic and diastolic blood pressure response to hydrochlorothiazide in Whites. PMID: 21127457
  69. The ability of beta-arrestins to play different scaffold functions would allow coordination of both Mdm2-dependent and -independent processes aimed at the specific modulation of GRK2 turnover in different signaling contexts PMID: 21081496
  70. findings indicated that platelet GRK2 and p-Ser670 GRK2 were reduced (36-41%) in unmedicated major depressive disorder subjects, and GRK2 content correlated inversely with the severity of depression PMID: 20493668
  71. desensitization of the dopamine D1-D2 receptor heteromer-mediated signal can occur by agonist occupancy even without activation and is dually regulated by both the catalytic and RGS domains of GRK2. PMID: 20807772
  72. Apoptosis and myocardial ischemia/reperfusion injury are found to be dependent on level of G protein-coupled receptor kinase-2. PMID: 20814022
  73. Studies seem to indicate that mild, soluble, Beta-amyloid accumulation can lead to a reduced membrane (functional) and an elevated cytosolic GRK2/5. PMID: 20730384
  74. GRK2 is an important negative regulator of insulin effects, key to the etiopathogenesis of insulin resistance and obesity. PMID: 20627936
  75. lymphocyte GRK2 levels are low after heart transplantation PMID: 20443948
  76. Enhanced GRK2 expression and desensitization of betaAR vasodilatation in hypertensive patients. PMID: 20443852
  77. The agonist-induced internalization of GPR109A receptors is regulated by GRK2 and arrestin3 in a pertussis toxin-sensitive manner and that internalized receptor recycling is independent of endosomal acidification. PMID: 20460384
  78. Prevention of GRK2 phosphorylation at S670 impedes normal GRK2 down-regulation and markedly delays cell cycle progression PMID: 20080565
  79. GRK2 mediates adrenergic insulin resistance and inhibition of GRK2 activity leads to increased insulin sensitivity both in cells and in animal model of insulin resistance. PMID: 19620130
  80. Data show that GRK2 stimulates the desensitization of GPR54 in HEK 293 cells and that beta-arrestin-2 mediates GPR54 activation of ERK1/2 in MDA-MB-231 cells. PMID: 19846537
  81. In cells overexpressing G protein-coupled receptor kinase 2 (GRK2), the thyrotropin-releasing hormone receptor is not phosphorylated. PMID: 19906838
  82. GRK2-phosphorylated recombinant ribosomal protein P2 reconstitutes translational activity of 60S ribosomal subunits and represents a potential novel signaling pathway responsible for P2 phosphorylation. PMID: 12379128
  83. a direct correlation between the expression of GRK2 and the desensitization of natively expressed H2 receptors in U-937 cells PMID: 12435819
  84. GRK2 plays a negative feedback regulatory role on protein kinase C(PKC)beta 1 activity in interaction between GRK2 and PKCbeta 1. PMID: 12456365
  85. identification of the amino-terminal domain as a regulatory Gbeta gamma binding site PMID: 12486133
  86. GRK2 is potential marker for organ injury and survival after cardiopulmonary bypass PMID: 12552191
  87. PDEG functions to link c-Src and G-protein-coupled receptor kinase 2 in a signaling unit that regulates p42/p44 mitogen-activated protein kinase by epidermal growth factor PMID: 12624098
  88. The pleckstsrin homology domain of this protein binds to PKC and affects the activity of PKC kinase. PMID: 12679936
  89. GRK2 requires agonist-induced formation of opioid receptor-G protein-coupled receptor kinase (GRK)-G beta gamma complex on the membrane in order to function PMID: 12750365
  90. GRK2 (and also GRK3, GRK5, and GRK6) is stabilized by interaction with Hsp90; GRK2 degradation induced by geldanamycin was predominantly through the proteasome pathway PMID: 14557268
  91. The concentration of betaARK1 in lymphocytes is greater in hypertensive individuals with left ventricular hypertrophy than in those without it PMID: 15097244
  92. GPRK2-mediated PDGFRbeta seryl phosphorylation plays an important role in desensitizing PDGFRbeta; this desensitization involves GPRK2-mediated phosphorylation of PDGFRbeta Ser(1104), with consequent dissociation of the PDGFRbeta from NHERF PMID: 15271984
  93. analysis of the GRK2 binding site of Galphaq PMID: 15471870
  94. role in terminating histamine H1 receptor singnaling by the kinase activity and RGS function of GRK2 PMID: 15542600
  95. beta-Arrestin 2 and GRK2 are potential mediators of signaling by activated Smoothened PMID: 15618519
  96. in leukocytes from patients with active relapsing-remitting multiple sclerosis (MS) or with secondary progressive MS, GRK2 levels are significantly reduced PMID: 15778405
  97. Ezrin is a novel substrate of GRK2 PMID: 15843435
  98. kinase binding to an mGluR1 domain involved in G protein-coupling is essential for the phosphorylation-independent attenuation of signaling by GRK2 PMID: 15870073
  99. the uncoupling and endocytosis of 5-HT4R require different GRK2 concentrations and involve distinct molecular events PMID: 15919661
  100. Overall, these data suggest that GRK2 has a regulatory role in EGF-induced ERK/MAPK activation. PMID: 16077899

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Subcellular Location Cytoplasm, Cell membrane
Protein Families Protein kinase superfamily, AGC Ser/Thr protein kinase family, GPRK subfamily
Tissue Specificity Expressed in peripheral blood leukocytes.
Database Links

HGNC: 289

OMIM: 109635

KEGG: hsa:156

STRING: 9606.ENSP00000312262

UniGene: Hs.83636

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