Recombinant Human Beta-adrenergic receptor kinase 1 (GRK2), partial

Code CSB-EP001394HU1
MSDS
Size $224
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  • (Tris-Glycine gel) Discontinuous SDS-PAGE (reduced) with 5% enrichment gel and 15% separation gel.
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Product Details

Purity
Greater than 90% as determined by SDS-PAGE.
Target Names
Uniprot No.
Research Area
Neuroscience
Alternative Names
ADRBK1; Adrenergic beta receptor kinase 1; ARBK1_HUMAN; BARK; BARK1; Beta adrenergic receptor kinase 1; Beta ARK 1; Beta ARK1; Beta-adrenergic receptor kinase 1; Beta-ARK-1; FLJ16718; G protein coupled receptor kinase 2; G-protein coupled receptor kinase 2; GRK2
Species
Homo sapiens (Human)
Source
E.coli
Expression Region
2-221aa
Target Protein Sequence
ADLEAVLADVSYLMAMEKSKATPAARASKKILLPEPSIRSVMQKYLEDRGEVTFEKIFSQKLGYLLFRDFCLNHLEEARPLVEFYEEIKKYEKLETEEERVARSREIFDSYIMKELLACSHPFSKSATEHVQGHLGKKQVPPDLFQPYIEEICQNLRGDVFQKFIESDKFTRFCQWKNVELNIHLTMNDFSVHRIIGRGGFGEVYGCRKADTGKMYAMKC
Note: The complete sequence including tag sequence, target protein sequence and linker sequence could be provided upon request.
Mol. Weight
29.6kDa
Protein Length
Partial
Tag Info
N-terminal 6xHis-tagged
Form
Liquid or Lyophilized powder
Note: We will preferentially ship the format that we have in stock, however, if you have any special requirement for the format, please remark your requirement when placing the order, we will prepare according to your demand.
Buffer
If the delivery form is liquid, the default storage buffer is Tris/PBS-based buffer, 5%-50% glycerol.
Note: If you have any special requirement for the glycerol content, please remark when you place the order.
If the delivery form is lyophilized powder, the buffer before lyophilization is Tris/PBS-based buffer, 6% Trehalose, pH 8.0.
Reconstitution
We recommend that this vial be briefly centrifuged prior to opening to bring the contents to the bottom. Please reconstitute protein in deionized sterile water to a concentration of 0.1-1.0 mg/mL.We recommend to add 5-50% of glycerol (final concentration) and aliquot for long-term storage at -20°C/-80°C. Our default final concentration of glycerol is 50%. Customers could use it as reference.
Troubleshooting and FAQs
Storage Condition
Store at -20°C/-80°C upon receipt, aliquoting is necessary for mutiple use. Avoid repeated freeze-thaw cycles.
Shelf Life
The shelf life is related to many factors, storage state, buffer ingredients, storage temperature and the stability of the protein itself.
Generally, the shelf life of liquid form is 6 months at -20°C/-80°C. The shelf life of lyophilized form is 12 months at -20°C/-80°C.
Lead Time
Delivery time may differ from different purchasing way or location, please kindly consult your local distributors for specific delivery time.
Notes
Repeated freezing and thawing is not recommended. Store working aliquots at 4°C for up to one week.
Datasheet & COA
Please contact us to get it.

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Target Background

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. Positively regulates ciliary smoothened (SMO)-dependent Hedgehog (Hh) signaling pathway by facilitating the trafficking of SMO into the cilium and the stimulation of SMO activity. Inhibits relaxation of airway smooth muscle in response to blue light.
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

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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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