Recombinant Human Beta-Adrenergic Receptor Kinase 1 (GRK2) Protein (His)

Name: Recombinant Human Beta-Adrenergic Receptor Kinase 1 (GRK2) Protein (His)
Brand: Beta LifeScience
SKU: BLC-08524P
Availability: InStock

Greater than 90% as determined by SDS-PAGE.

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Product Overview

Description	Recombinant Human Beta-Adrenergic Receptor Kinase 1 (GRK2) Protein (His) is produced by our E.coli expression system. This is a protein fragment.
Purity	Greater than 90% as determined by SDS-PAGE.
Uniprotkb	P25098
Target Symbol	GRK2
Synonyms	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)
Expression System	E.coli
Tag	N-6His
Target Protein Sequence	ADLEAVLADVSYLMAMEKSKATPAARASKKILLPEPSIRSVMQKYLEDRGEVTFEKIFSQKLGYLLFRDFCLNHLEEARPLVEFYEEIKKYEKLETEEERVARSREIFDSYIMKELLACSHPFSKSATEHVQGHLGKKQVPPDLFQPYIEEICQNLRGDVFQKFIESDKFTRFCQWKNVELNIHLTMNDFSVHRIIGRGGFGEVYGCRKADTGKMYAMKC
Expression Range	2-221aa
Protein Length	Partial
Mol. Weight	29.6kDa
Research Area	Neuroscience
Form	Liquid or Lyophilized powder
Buffer	Liquid form: default storage buffer is Tris/PBS-based buffer, 5%-50% glycerol. Lyophilized powder form: the buffer before lyophilization is Tris/PBS-based buffer, 6% Trehalose, pH 8.0.
Reconstitution	Briefly centrifuged the vial prior to opening to bring the contents to the bottom. Reconstitute protein in deionized sterile water to a concentration of 0.1-1.0 mg/mL. It is recommended to add 5-50% of glycerol (final concentration) and aliquot for long-term storage at -20°C/-80°C. The default final concentration of glycerol is 50%.
Storage	1. Store at -20°C/-80°C upon receipt, aliquoting is necessary for mutiple use. 2. Avoid repeated freeze-thaw cycles. 3. Store working aliquots at 4°C for up to one week. 4. In general, protein in liquid form is stable for up to 6 months at -20°C/-80°C. Protein in lyophilized powder form is stable for up to 12 months at -20°C/-80°C.
Notes	Repeated freezing and thawing is not recommended. Store working aliquots at 4°C for up to one week.

Target Details

Target 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.
Subcellular Location	Cytoplasm. Cell membrane.
Protein Families	Protein kinase superfamily, AGC Ser/Thr protein kinase family, GPRK subfamily
Database References	HGNC: 289 OMIM: 109635 KEGG: hsa:156 STRING: 9606.ENSP00000312262 UniGene: PMID: 29864421 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 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 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 KHSV miR-K3 activates the GRK2/CXCR2/AKT axis inducing KSHV-induced angiogenesis and promoting KSHV latency. PMID: 27058419 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 Low grk2 expression is associated with lung metastasis in gastric cancer. PMID: 28843497 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 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 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 The tyrosine-phosphorylated GRK2 mediates this inhibition by acting on the second intracellular loop of D3R. PMID: 28579429 GRK2 is overexpressed in pancreatic cancer, and might serve as a potential indicator of unfavorable prognosis. PMID: 27346572 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 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 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 GRK2 may inhibit IGF1-induced human hepatocellular carcinoma cell growth and migration through downregulation of EGR1. PMID: 26936374 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 Suggest role for GRK2 in the regulating cardiac hypertrophy. PMID: 26224342 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 Acute mental stress significantly increased GRK2 density in in peripheral blood mononuclear cells of young adult males. PMID: 26706289 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 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 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 G protein beta subunits (Gb) bind to DDB1 and Gb2 targets GRK2 for ubiquitylation by the DDB1-CUL4A-ROC1 ubiquitin ligase. PMID: 25982117 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 Knockdown of ADRBK1 gene has detrimental effects on breast cancer cell growth. PMID: 25279970 Results uncovered that Gaq binding to GRK2 enhances the recruitment of GRK2 to M3-ACh receptors. PMID: 25316767 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 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 Low levels of GRK2/GRK5 causes a slow and not complete desensitization/down-regulation of GPR17. PMID: 24613411 GRK2 is localized to centrosomes and plays a central role in mitogen-promoted centrosome separation. PMID: 23904266 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 Changes in lymphocyte GRK2 after exercise training can strongly predict outcome in advanced heart failure. PMID: 23689525 This review discusses recently discovered roles of GRK2 as a biomarker in cardiomyocyte metabolism and myocardial contraction. PMID: 24812353 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 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 Desensitization and internalization of endothelin receptor A: impact of G protein-coupled receptor kinase 2 (GRK2)-mediated phosphorylation. PMID: 24064210 Data indicate that CXCL12-induced phosphorylation at CXCR4 S346/347 was mediated by GRK2/3. PMID: 23734232 GRK2 takes part in the regulation of the initial inflammatory response during mycobacterial infection. PMID: 23312955 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 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 Gene transfer of human GRK2 inhibitory peptide preserved regional/global systolic function after acute MI without arresting progressive ventricular remodeling. PMID: 23208013 This study identify that GRK2 as a potential molecular link between inflammation and mGluR-mediated sensitization. PMID: 23494575 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 Increased localization is seen in heart mitochondria from cardiac-specific GRK2 transgenic mice compared with normal littermate controls. PMID: 23467820 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 Persistent hyperalgesia in GRK2-deficient mice is associated with an increase in spinal cord microglia/macrophages. PMID: 22731384 Inhibition of G-protein-coupled receptor kinase 2 (GRK2) triggers the growth-promoting mitogen-activated protein kinase (MAPK) pathway PMID: 23362259 a novel role for IL-8 in inhibiting betaAR agonist-stimulated alveolar epithelial fluid transport via GRK2/PI3K-dependent mechanisms. PMID: 23221335 These data suggest cell type- and subcellular compartment-dependent differences in GRK/arrestin-mediated desensitization and signaling. PMID: 23139825

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Proteins are sensitive to heat, and freeze-drying can preserve the activity of the majority of proteins. It improves protein stability, extends storage time, and reduces shipping costs. However, freeze-drying can also lead to the loss of the active portion of the protein and cause aggregation and denaturation issues. Nonetheless, these adverse effects can be minimized by incorporating protective agents such as stabilizers, additives, and excipients, and by carefully controlling various lyophilization conditions.

Commonly used protectant include saccharides, polyols, polymers, surfactants, some proteins and amino acids etc. We usually add 8% (mass ratio by volume) of trehalose and mannitol as lyoprotectant. Trehalose can significantly prevent the alter of the protein secondary structure, the extension and aggregation of proteins during freeze-drying process; mannitol is also a universal applied protectant and fillers, which can reduce the aggregation of certain proteins after lyophilization.

Our protein products do not contain carrier protein or other additives (such as bovine serum albumin (BSA), human serum albumin (HSA) and sucrose, etc., and when lyophilized with the solution with the lowest salt content, they often cannot form A white grid structure, but a small amount of protein is deposited in the tube during the freeze-drying process, forming a thin or invisible transparent protein layer.

Reminder: Before opening the tube cap, we recommend that you quickly centrifuge for 20-30 seconds in a small centrifuge, so that the protein attached to the tube cap or the tube wall can be aggregated at the bottom of the tube. Our quality control procedures ensure that each tube contains the correct amount of protein, and although sometimes you can't see the protein powder, the amount of protein in the tube is still very precise.

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