CXCR4 Human Chemokine GPCR Cell Based Antagonist Total Internalization LeadHunter Assay - US

Background Information:

CXCR4 (CXC Chemokine Receptor 4), also called fusin, is an alpha-chemokine receptor specific for stromal-derived-factor-1 (SDF-1 also called CXCL12), a molecule endowed with potent chemotactic activity for lymphocytes. It is highly expressed in brain and heart, and in white blood cells, vascular endothelial cells, umbilical cord endothelial cells, and several tumor cell lineages. This receptor is an HIV-1 fusion co-factor that allows HIV-1 invasion in diverse human cell types. CXCR4 is involved in organ vascularization, neuronal cell migration, and patterning of the central nervous system during development.

PathHunter Total GPCR Internalization cell lines are engineered to co-express the ProLink™ (PK) tagged GPCR, and an Enzyme Acceptor (EA) tag localized to the plasma membrane. Membrane bound, PK-tagged receptors are in close proximity to the EA, forcing complementation of the two β-galactosidase enzyme fragments (EA and PK). The resulting functional enzyme hydrolyzes substrate to generate a high basal chemiluminescent signal. Activation of the GPCR-PK induces internalization of the receptor, which dissociates the EA/PK complementation, and results in a loss of chemiluminescent signal.

Family:

GPCR

Sub Family:

Chemokine

Class:

Class A

Coupling:

Gi/Go

Protein Name:

CXCR4

Uniprot Number:

P61073

Protein Aliases:

CXCR-4|Fusin|Leukocyte-derived seven transmembrane domain receptor|LESTR|Pre-B-cell-derived chemokine receptor|PB-CKR|Stromal cell-derived factor 1 receptor|SDF-1 receptor|CD antigen CD184

Gene Name:

CXCR4

Gene ID:

7852

Gene Aliases:

LESTR|NPY3R|HM89|NPYY3R|D2S201E|fusin|HSY3RR|NPYR|CD184

Accession Number:

AY242129

Organism:

Human

Cell Type:

U2OS