The chemokine receptor CXCR4 is a widely expressed G protein-coupled receptor required for development, hematopoiesis, organogenesis, and vascularization. In disease, CXCR4 has been implicated in WHIM syndrome, HIV, and cancers. Regulation of CXCR4 function occurs through phosphorylation at multiple sites in the C-terminal region. These sites have been shown to be phosphorylated after CXCL12 stimulation, and involve several kinases, such as PKC and GRK kinases. After CXCL12 stimulation of HEK293 cells, Ser-324 and Ser-325 become phosphorylated by PKC and GRK6, while Ser-330 and Ser-339 are phosphorylated by only GRK6. In human astroglia cells, Ser-324 and Ser-325 are rapidly phosphorylated in endogenous CXCR4, while Ser-330 was phosphorylated with slower kinetics. In addition, arrestin binding to CXCR4 is driven by this phosphorylation of far C-terminal residues. Thus, site-specific phosphorylation of CXCR4 may be regulated by multiple kinases lead to complex regulation of CXCR4 signaling.
Bhandari, D. et al. (2009) Mol Biol Cell. 20:1324.
Orsini, M.J. et al. (2000) J Biol Chem. 275(33):25876.
Orsini, M.J. et al. (1999) J Biol Chem. 274(43):31076.
*For more information, see UniProt Accession P61073
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*All molecular weights (MW) are confirmed by comparison to Bio-Rad Rainbow Markers and to western blot mobilities of known proteins with similar MW.
This kit contains: