GRK5 / GPRK5 recombinant protein

Recombinant Human GRK5 / GPRK5 Protein (His tag)

Cat. Num. AAA2546054

• Gene Names: GRK5; GPRK5
• Purity: > 90 % as determined by SDS-PAGE
• Synonyms: GRK5 / GPRK5; Recombinant Human GRK5 / GPRK5 Protein (His tag); FLJ39780; GPRK5; GRK5 / GPRK5 recombinant protein

• Host: Baculovirus-Insect Cells
• Purity/Purification: > 90 % as determined by SDS-PAGE
• Form/Format: Lyophilized from sterile 50mM Tris, 100mM NaCl, 0.5mM PMSF, 1mM DTT, 0.5mM EDTA, 10% gly, pH 7.4
• Sequence Length: 590

• Application Notes: The recombinant human GRK5 consists of 600 amino acids and predicts a molecular mass of 69 kDa. The apparent molecular mass of rhGRK5 is approximately 58 kDa in SDS-PAGE under reducing conditions.
• Predicted N Terminal: Met 1
• 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 GRK5 / GPRK5 recombinant protein

Background: G protein-coupled receptor kinase 5, also known as G protein-coupled receptor kinase GRK5 and GRK5, is a member of the protein kinase superfamily, AGC Ser/Thr protein kinase family and GPRK subfamily. GRKs specifically phosphorylate agonist-occupied G protein-coupled receptors at the inner surface of the plasma membrane (PM), leading to receptor desensitization. GRKs utilize a variety of mechanisms to bind tightly, and sometimes reversibly, to cellular membranes. GRKs play an important role in mediating agonist-specific desensitization of numerous G protein-coupled receptors. GRK5 contains one AGC-kinase C-terminal domain, one protein kinase domain and one RGS domain. GRK5 specifically phosphorylates the activated forms of G protein-coupled receptors. Phospholipid-stimulated autophosphorylation may represent a novel mechanism for membrane association and regulation of GRK5 activity. GRK5 deficiency significantly exaggerates microgliosis and astrogliosis in the presence of an inflammatory initiator, such as the excess fibrillar Abeta and the subsequent active inflammatory reactions. GRK5 deficiency has been linked to early Alzheimer's disease in humans and mouse models of the disease.

Description: A DNA sequence encoding the human GRK5 (NP_005299.1) (Met 1-Ser 590) was fused with a polyhistidine tag at the C-terminus.

NCBI and Uniprot Product Information

• NCBI GI #: 4885349
• NCBI GeneID: 2869
• NCBI Accession #: NP_005299.1
• NCBI GenBank Nucleotide #: NM_005308.2
• UniProt Accession #: P34947; Q5T059; D3DRD0
• Molecular Weight: 67,787 Da
• NCBI Official Full Name: G protein-coupled receptor kinase 5
• NCBI Official Synonym Full Names: G protein-coupled receptor kinase 5
• NCBI Official Symbol: GRK5
• NCBI Official Synonym Symbols: GPRK5
• NCBI Protein Information: G protein-coupled receptor kinase 5
• UniProt Protein Name: G protein-coupled receptor kinase 5
• UniProt Gene Name: GRK5
• UniProt Synonym Gene Names: GPRK5

NCBI Description

This gene encodes a member of the guanine nucleotide-binding protein (G protein)-coupled receptor kinase subfamily of the Ser/Thr protein kinase family. The protein phosphorylates the activated forms of G protein-coupled receptors thus initiating their deactivation. It has also been shown to play a role in regulating the motility of polymorphonuclear leukocytes (PMNs). [provided by RefSeq, Jul 2008]

Uniprot Description

GRK5: Serine/threonine kinase that phosphorylates preferentially the activated forms of a variety of G-protein- coupled receptors (GPCRs). Such receptor phosphorylation initiates beta-arrestin-mediated receptor desensitization, internalization, and signaling events leading to their down-regulation. Phosphorylates a variety of GPCRs, including adrenergic receptors, muscarinic acetylcholine receptors (more specifically Gi-coupled M2/M4 subtypes), dopamine receptors and opioid receptors. In addition to GPCRs, also phosphorylates various substrates: Hsc70- interacting protein/ST13, TP53/p53, HDAC5, and arrestin-1/ARRB1. Phosphorylation of ARRB1 by GRK5 inhibits G-protein independent MAPK1/MAPK3 signaling downstream of 5HT4-receptors. Phosphorylation of HDAC5, a repressor of myocyte enhancer factor 2 (MEF2) leading to nuclear export of HDAC5 and allowing MEF2- mediated transcription. Phosphorylation of TP53/p53, a crucial tumor suppressor, inhibits TP53/p53-mediated apoptosis. Phosphorylation of ST13 regulates internalization of the chemokine receptor. Phosphorylates rhodopsin (RHO) (in vitro) and a non G- protein-coupled receptor, LRP6 during Wnt signaling (in vitro). Belongs to the protein kinase superfamily. AGC Ser/Thr protein kinase family. GPRK subfamily.

Protein type: AGC group; EC 2.7.11.16; GRK family; GRK subfamily; Kinase, protein; Protein kinase, AGC; Protein kinase, Ser/Thr (non-receptor)

Chromosomal Location of Human Ortholog: 10q26.11

Cellular Component: cytoplasm; focal adhesion; nuclear membrane; nucleus; plasma membrane

Molecular Function: beta-adrenergic receptor kinase activity; phospholipid binding; protein binding; protein kinase C binding; protein serine/threonine kinase activity

Biological Process: G-protein signaling, coupled to cAMP nucleotide second messenger; negative regulation of apoptosis; positive regulation of cell proliferation; protein amino acid autophosphorylation; regulation of cell cycle; regulation of G-protein coupled receptor protein signaling pathway; tachykinin signaling pathway