Biological Information

Background Information:

Chemokine receptors belong to the superfamily of G protein-coupled seven transmembrane proteins. G-protein-coupled receptors constitute one of the major signal transduction systems in eukaryotic cells. Coding sequences for these receptors, in those regions believed to contribute to the agonist-antagonist binding site, are strongly conserved across mammalian species. Chemokine receptors are primarily distributed on cells involved in immune and inflammatory function. CX3CR1 isoforms were found to serve as a coreceptors for HIV-1 and HIV-2 envelope fusion and virus infection. CX3CR1 mediates leukocyte migration and adhesion.

PathHunter β-Arrestin GPCR cell lines are engineered to co-express the ProLink™ (PK) tagged GPCR and the Enzyme Acceptor (EA) tagged β-Arrestin. Activation of the GPCR-PK induces β-Arrestin-EA recruitment, forcing complementation of the two β-galactosidase enzyme fragments (EA and PK). The resulting functional enzyme hydrolyzes substrate to generate a chemiluminescent signal.

Family:

GPCR

Sub Family:

Chemokine

Class:

Class A

Coupling:

Gi/Go

Protein Name:

CX3CR1

Uniprot Number:

Q9Z0D9

Protein Aliases:

CX3CR1|Beta chemokine receptor-like 1|CMK-BRL-1|CMK-BRL1|Fractalkine receptor|G-protein coupled receptor 13|V28

Gene Name:

CX3CR1

Gene ID:

13051

Gene Aliases:

CMKDR1|V28|CCRL1|CMKBRL1|GPR13

Accession Number:

NM_009987.3

Organism:

Mouse

Cell Type:

CHO-K1

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Antagonist

β-Arrestin Isoform:

β-Arrestin-2

Testing Information

Control Activator:

Human Fractalkine(CX3CL1)

Test Concentration / Dose:

Eurofins will provide IC/EC50 calculation if 10 concentrations are selected

Test Sample Requirements:

40uL of a 1000X stock for the first assay and 2uL for each additional assay (assay = 1 target, 1 readout, 1 mode)

Minimum Order Quantity:

20

Turnaround Time

Standard:

15 Business Days

Clinical Relevance

Adverse / Beneficial Action:

Antagonism of CX3CR1 may be useful in the treatment of atherosclerosis, diabetic nephropathy, rheumatoid arthritis, allodynia and various allergies (asthma, dermatitis, rhinitis).

Additional Information

Brand:

LeadHunter

Testing Location:

USA - Fremont, CA