GRK2 / ADRBK1 recombinant protein

Recombinant Human GRK2 / ADRBK1 Protein (His & GST tag)

Cat. Num. AAA2545675

• Gene Names: GRK2; BARK1; ADRBK1; BETA-ARK1
• Purity: > 90 % as determined by SDS-PAGE
• Synonyms: GRK2 / ADRBK1; Recombinant Human GRK2 / ADRBK1 Protein (His & GST tag); ADRBK1; BARK1; BETA-ARK1; FLJ16718; GRK2; GRK2 / ADRBK1 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, pH 8.0
• Sequence Length: 689

• Application Notes: The recombinant human ADRBK1/GST chimera consists of 926 amino acids and has a calculated molecular mass of 107 kDa. It migrates as an approximately 110 kDa band in SDS-PAGE under reducing conditions.
• Predicted N Terminal: Met
• Endotoxin: < 1.0 EU per mug of the protein as determined by the LAL method
• Preparation and Storage: Samples are stable for up to twelve months from date of receipt at -70 degree C

SDS-PAGE

Related Product Information for GRK2 / ADRBK1 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.

Description: 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.

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: G protein-coupled receptor kinase 2
• NCBI Official Symbol: GRK2
• NCBI Official Synonym Symbols: BARK1; ADRBK1; BETA-ARK1
• NCBI Protein Information: beta-adrenergic receptor kinase 1
• UniProt Protein Name: Beta-adrenergic receptor kinase 1
• UniProt Gene Name: GRK2
• UniProt Synonym Gene Names: Beta-ARK-1

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

Chromosomal Location of Human Ortholog: 11q13.2

Cellular Component: cytoplasm; cytosol; membrane; plasma membrane

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

Biological Process: acetylcholine receptor signaling, muscarinic pathway; cardiac muscle contraction; desensitization of G-protein coupled receptor protein signaling pathway; entry of virus into host cell; negative regulation of striated muscle contraction; negative regulation of the force of heart contraction by chemical signal; peptidyl-serine phosphorylation; positive regulation of catecholamine secretion; receptor internalization; tachykinin signaling pathway; viral genome replication