- Catalog number
- PB9708
- Size / count
- 100 µg/Vial
- Dry ice
- No
- Hazardous
- No
- Discontinued
- No
- Background
- G protein-coupled receptor kinase 5?is an?enzyme?that in humans is encoded by the?GRK5?gene. It is mapped to 10q26.11. 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) .
- Synonyms
- G protein-coupled receptor kinase 5;2.7.11.16; G protein-coupled receptor kinase GRK5; GRK5; GPRK5
- Gene Name
- GRK5
- Gene ID
- 2869
- UniProt
- P34947
- Host
- Rabbit
- Reactivity
- Human, Mouse, Rat
- Cross Reactivity
- No cross-reactivity with other proteins
- Immunogen
- A synthetic peptide corresponding to a sequence at the C-terminus of human GRK5, different from the related mouse and rat sequences by three amino acids.
- Clonality
- Polyclonal
- Tissue Specificity
- Highest levels in heart, placenta, lung > skeletal muscle > brain, liver, pancreas > kidney. .
- Applications
- IHC, WB
- Field of Research
- Atherosclerosis, Cardiovascular, G Protein Signaling, Heterotrimeric G Proteins, Protein Phosphorylation, Ser/Thr Kinases, Signal Transduction, Signaling Pathway, Vascular Inflammation
- Purification
- Immunogen affinity purified.
- Concentration
- Adding 0.2 ml of distilled water will yield a concentration of 500 μg/ml.
- Form
- Lyophilized
- Reconstitution
- Add 0.2ml of distilled water will yield a concentration of 500ug/ml.
- Function
- 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) . .
- References & Citations
- 1. Entrez Gene: GRK5 G protein-coupled receptor kinase 5. 2. Bullrich F, Druck T, Kunapuli P, et al. (1995) . Chromosomal mapping of the genes GPRK5 and GPRK6 encoding G protein-coupled receptor kinases GRK5 and GRK6.. Cytogenet. Cell Genet. 70 (3–4) : 250–4. 3. Kunapuli P, Benovic JL (Jul 1993) . Cloning and expression of GRK5: a member of the G protein-coupled receptor kinase family. Proc Natl Acad Sci U S A 90 (12) : 5588–92.
- Storage Conditions
- Store at -20°C for one year from date of receipt. After reconstitution, at 4°C for one month. It can also be aliquotted and stored frozen at -20°C for six months. Avoid repeated freeze-thaw cycles.
- Calculated Molecular Weight
- 67787 MW
- Observed Molecular Weight
- 68 kDa
- Specificity
- No cross reactivity with other proteins.
- Gene Name Synonym
- G protein-coupled receptor kinase 5
- Subcellular Location
- Cytoplasm. Nucleus. Cell membrane; Peripheral membrane protein. Predominantly localized at the plasma membrane; targeted to the cell surface through the interaction with phospholipids. Nucleus localization is regulated in a GPCR and Ca (2+) /calmodulin-dependent fashion.
- Protein Name
- G protein-coupled receptor kinase 5
- Isotype
- Rabbit IgG
- Contents
- Each vial contains 5mg BSA, 0.9mg NaCl, 0.2mg Na2HPO4, 0.05mg NaN3.