GRK5, active, Recombinant, Human (G Protein-Coupled Receptor Kinase 5)

G protein-coupled receptor kinases (GRKs) play an important role in phosphorylating and regulating the activity of a variety of G protein-coupled receptors. GRK5 is a Ser/Thr protein kinase and a member of the guanine nucleotide-binding protein GRK subfamily. Itphosphorylates the activated forms of GRKs which initiates their deactivation. It has also been shown to play a role in regulating the motility of polymorphonuclear leukocytes (PMNs). Desensitization of GRKs regulates the number of PMNs, as well as their motility and ability to stop upon contact with\npathogens or target cells (3). MIP2 induces GRK2 and GRK5 expression in PMNs through PI3KG \nsignaling. However, lipopolysaccharide (LPS), acting through TLR4, and mediated through MEK1/2, transcriptionally downregulates expression of GRK2 and GRK5 in response to MIP2. This decreases chemokine receptor desensitization and markedly augments PMN migration. Thus, LPS-activated TLR4 signaling regulates PMN migration by modulating the expression of chemokine receptors in a GRK2- and GRK5-dependent manner (1-3). \n\nSpecific Activity: 28nmol/min/mg\n \nActivity Assay: \nKinase activity is measured as the molar amount of phosphate incorporated into Casein per minute per mg protein at 30 degrees C using a final concentration of 50uM [32P] ATP.\n\nStorage and Stability:\nMay be stored at 4 degrees C for short-term only. For long-term storage, aliquot to avoid repeated freezing and thawing and freeze at -70 degrees C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Aliquots are stable for at least 12 months.

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SPECIFICATIONS

Catalog Number

G8972-20

Size

5ug

Form

Supplied in 50mM Tris-HCl, pH 7.5, 150mM sodium chloride, 0.25mM DTT, 0.1mM EGTA, 0.1mM EDTA, 0.1mM PMSF, 25% glycerol.

Purity

(same/more than) 90% as determined by SDS-PAGE analysis.

References

1. Haribabu, B.; Snyderman, R (1993) Proc. Nat. Acad. Sci. 90: 9398-9402. \n2. Bullrich, F.; Druck, T.; Kunapuli, P.; Gomez, J.; Gripp, K. W.; Schlegelberger, B.; Lasota, J.;\nAronson, M.; Cannizzaro, L. A.; Huebner, K.; Benovic, J. L. (1996) Cytogenet. Cell Genet. 70: 250-254. \n3. Fan, J.; Malik, A. B (2003) Nature Med. 9: 315-321. \n