ChemiScreen™ CXCR2 Membrane Preparation

ChemiScreen™ CXCR2 Membrane Preparation

• ChemiScreen
• Chemicon (Millipore)

200 assays

TRANSFECTION: Full-length human CXCR2 cDNA (Accession Number: M73969)

CXCR2 is a 7-TM G-protein coupled receptor that binds to the chemokines GROalpha, GRObeta, GROgamma, IL-8, ENA-78, NAP-2 and GCP-2 (Olson and Ley, 2002). Neutrophils, mast cells and microvascular endothelial cells express CXCR2, and interactions of CXCR2 with its ligands promotes chemotaxis of these cell types (Heidemann et al., 2003; Nilsson et al., 1999; White et al., 1998). Studies with mice lacking CXCR2 indicate that CXCR2 promotes growth of primary tumors and secondary metastases (Keane et al., 2004), and plays an essential role in hyperoxia-induced lung injury (Sue et al., 2004). In addition, cytomegalovirus encodes a CXCR2-binding chemokine, vCXC-1, that promotes neutrophil migration to infected cells (Penfold et al., 1999). Chemicon's CXCR2 Membrane Preps are ideal tools for screening for antagonists of interactions between CXCR2 and its ligands. Radiolabeled IL-8 binds to the CXCR2 membranes with a Kd of 0.075 nM. With 0.1 nM 125I-labeled IL-8, a 5-fold window of specific binding is obtained.

Radioligand binding assay.

Human

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The protein encoded by this gene is a member of the G-protein-coupled receptor family. This protein is a receptor for interleukin 8 (IL8). It binds to IL8 with high affinity, and transduces the signal through a G-protein activated second messenger system. This receptor also binds to chemokine (C-X-C motif) ligand 1 (CXCL1/MGSA), a protein with melanoma growth stimulating activity, and has been shown to be a major component required for serum-dependent melanoma cell growth. This receptor mediates neutrophil migration to sites of inflammation. The angiogenic effects of IL8 in intestinal microvascular endothelial cells are found to be mediated by this receptor. Knockout studies in mice suggested that this receptor controls the positioning of oligodendrocyte precursors in developing spinal cord by arresting their migration. This gene, IL8RA, a gene encoding another high affinity IL8 receptor, as well as IL8RBP, a pseudogene of IL8RB, form a gene cluster in a region mapped to chromosome 2q33-q36.

FUNCTION: SwissProt: P25025 # Receptor to interleukin-8, which is a powerful neutrophils chemotactic factor. Binding of IL-8 to the receptor causes activation of neutrophils. This response is mediated via a G-protein that activate a phosphatidylinositol-calcium second messenger system. This receptor binds to IL-8 with a high affinity and to GRO/MGSA and NAP-2 also with a high affinity.
SIZE: 360 amino acids; 40759 Da
SUBCELLULAR LOCATION: Cell membrane; Multi-pass membrane protein.
PTM: Phosphorylated upon ligand binding; which is required for desensitization.
SIMILARITY: SwissProt: P25025 ## Belongs to the G-protein coupled receptor 1 family.

Human

Chemicon

CXCR2 / IL-8b

Membranes were adjusted to 0.5 mg protein/ml in 50 mM Tris pH 7.4, 10% glycerol and 1% BSA, rapidly frozen, and stored at -80°C. One vial typically contains 1000 units, where a unit is the amount of membrane that will yield greater than 1000 cpm specific binding of 125I-labeled IL-8 (0.1 nM input concentration).

peptide

Maintain frozen at -70°C for up to 2 years. Do not freeze and thaw.

Chemokine

A

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• IL8RB
• CD182
• CMKAR2
• CXCR-2
• IL8RA
• IL8R2
• CXCR2
• CDw128b

GPCR Membrane Preparations

ChemiScreen™ CXCR2 Membrane Preparation

0.5 mg/mL

Bmax for [¹²⁵I]IL-8 binding: 0.93 pmol/mg protein; Kd for [¹²⁵I] IL-8 binding: ~ 0.075 nM

Chem-1

Chem-1

Membranes

P25025

NM_001557.2

GPCR