GRK2 recombinant protein

GRK2 Protein, Human, Recombinant (His & GST Tag)

Cat. Num. AAA8120964

• Gene Names: ADRBK1; GRK2; BARK1; BETA-ARK1
• Purity: >90% as determined by SDS-PAGE
• Synonyms: GRK2; GRK2 Protein; Human; Recombinant (His & GST Tag); Human GRK2/ADRBK1 Protein (His & GST Tag); adrenergic; beta; receptor kinase 1; GRK2 recombinant protein

• Host: Baculovirus-Insect Cells
• Purity/Purification: >90% as determined by SDS-PAGE
• Form/Format: Lyophilized from sterile 50mM Tris, 500mM NaCl, 0.5mM GSH, pH8.0. Normally 5%-8% trehalose, mannitol and 0.01% Tween80 are added as protectants before lyophilization. Please refer to the specific buffer information in the hard copy of CoA.
• Sequence: Met1-Leu689

• Species: Human
• Activity: No Kinase Activity
• Endotoxin: <1.0EU per ug of the protein as determined by the LAL method
• Predicted N Terminal: Met
• Tag: N-GST & His
• Protein Construction: A DNA sequence encoding the human ADRBK1 (NP_001610.2)(Met 1-Leu 689) was fused with the N-terminal polyhistidine-tagged GST tag at the N-terminus.
• Reconstitution: A hardcopy of COA with reconstitution instruction is sent along with the products. Please refer to it for detailed information.
• Preparation and Storage: Samples are stable for up to twelve months from date of receipt at -20 degree C to -80 degree C. Store it under sterile conditions at -20 degree C to -80 degree C. It is recommended that the protein be aliquoted for optimal storage. Avoid repeated freeze-thaw cycles.; In general, recombinant proteins are provided as lyophilized powder which are shipped at ambient temperature. Bulk packages of recombinant proteins are provided as frozen liquid.; They are shipped out with blue ice.

SDS-Page

Related Product Information for GRK2 recombinant protein

Background: 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.

References

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.

NCBI and Uniprot Product Information

• NCBI GI #: 148539876
• NCBI GeneID: 156
• NCBI Accession #: NP_001610.2
• NCBI GenBank Nucleotide #: NM_001619.3
• UniProt Accession #: P25098; Q13837; Q6GTT3; B0ZBE1
• Molecular Weight: 79,574 Da
• NCBI Official Full Name: beta-adrenergic receptor kinase 1
• NCBI Official Synonym Full Names: adrenergic, beta, receptor kinase 1
• NCBI Official Symbol: ADRBK1
• NCBI Official Synonym Symbols: GRK2; BARK1; BETA-ARK1
• NCBI Protein Information: beta-adrenergic receptor kinase 1; beta-ARK-1; G-protein coupled receptor kinase 2
• UniProt Protein Name: Beta-adrenergic receptor kinase 1
• Protein Family: Beta-adrenergic receptor kinase
• UniProt Gene Name: ADRBK1
• UniProt Synonym Gene Names: BARK; BARK1; GRK2; Beta-ARK-1
• UniProt Entry Name: ARBK1_HUMAN

NCBI Description

The product of this gene phosphorylates the beta-2-adrenergic receptor and appears to mediate agonist-specific desensitization observed at high agonist concentrations. This protein 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]

Uniprot Description

GRK2: a ubiquitous protein kinase of the GRK family. Phosphorylates the beta-2-adrenergic receptor and related G-protein-coupled receptors. Appears to mediate agonist-specific desensitization observed at high agonist concentrations. Expression level is consistently elevated in chronic human heart failure. Mouse models of severe heart failure have been used to demonstrate that inhibition of BARK1 with a peptide inhibitor is sufficient to increase mean survival, reduce dialation and improve cardiac function.

Protein type: Protein kinase, AGC; Protein kinase, Ser/Thr (non-receptor); Kinase, protein; EC 2.7.11.15; AGC group; GRK family; BARK subfamily

Chromosomal Location of Human Ortholog: 11q13.1

Cellular Component: membrane; cytoplasm; plasma membrane; cytosol

Molecular Function: G-protein coupled receptor kinase activity; protein binding; Edg-2 lysophosphatidic acid receptor binding; beta-adrenergic receptor kinase activity; alpha-2A adrenergic receptor binding; ATP binding; protein kinase activity

Biological Process: epidermal growth factor receptor signaling pathway; desensitization of G-protein coupled receptor protein signaling pathway; tachykinin signaling pathway; acetylcholine receptor signaling, muscarinic pathway; fibroblast growth factor receptor signaling pathway; nerve growth factor receptor signaling pathway; heart development; peptidyl-threonine phosphorylation; signal transduction; negative regulation of striated muscle contraction; peptidyl-serine phosphorylation; negative regulation of the force of heart contraction by chemical signal; phospholipase C activation; receptor internalization; positive regulation of catecholamine secretion; innate immune response; cardiac muscle contraction