HUMAN RECOMBINANT CXCR2 RECEPTOR
MULTISCREEN™ STABLE CELL LINES
1 vial (2 x 106) frozen cells
Sigma Freezing Medium (C-6164)
Expression vector containing full-length human CXCR2 cDNA (GenBank Accession Number NM_001557) with FLAG tag sequence at N-terminus
Liquid nitrogen upon receiving
Propagation Medium: DMEM, 10% FBS, 1 μg/mL puromycin
Stable in culture for minimum of two months
Background: CXCR2 (high affinity interleukin-8 receptor B, IL8RB) is a receptor to interleukin-8, which is a powerful neutrophil chemotactic factor. Binding of IL-8 to the receptor causes activation of neutrophils. This receptor also binds to GRO/MGSA and NAP-2 with high affinity. Some highly potent small molecule antagonists of CXCR2 showed success in blocking in vivo trafficking of neutrophils, suggesting that antagonism of IL-8 at the receptor level is a viable therapeutic strategy in conditions such as pulmonary disease.
Application: Functional assays
Figure 1. Dose-dependent stimulation of calcium flux upon treatment with ligand, measured with MultiscreenTM Calcium 1.0 No Wash Assay Kit (Multispan MSCA01). Figure 2. Dose-dependent inhibition of forskolin-stimulated intracellular cAMP accumulation upon treatment with ligand, measured with MultiscreenTM TR-FRET cAMP 1.0 No Wash Assay Kit (Multispan MSCM01). Figure 3. Receptor expression on cell surface measured by flow cytometry (FACS) using an anti-FLAG antibody. Thin line: parental cells; thick line: receptor-expressing cells.
Sprenger et al. (1994) Structure, genomic organization, and expressionof the human interleukin-8 receptor B gene. J Biol Chem 269:11065-11072.
Pease and Sabroe (2002) The role of interleukin-8 and its receptors in inflammatory lung disease: implications for therapy. Am J Respir Med 1:19-25.