C-X-C chemokine receptor type 4 (CXCR4), also known as fusin or CD184 (cluster of differentiation 184), is a chemokine receptor with several aliases, including CXCR4, CD184, D2S201E, FB22, HM89, HSY3RR, LAP3, LCR1, LESTR, NPY3R, NPYR, NPYRL, NPYY3R, and WHIM. CXCR4 specifically binds to stromal-derived factor-1 (SDF-1, also known as CXCL12), a molecule with strong chemotactic properties for lymphocytes.
This receptor plays a critical role in HIV infection, as some HIV isolates use CXCR4 to infect CD4+ T cells, typically referred to as T-cell tropic isolates. These viruses are often observed later in the infection process, and it remains uncertain whether the appearance of CXCR4-utilizing HIV strains is a cause or a result of immunodeficiency.
CXCR4 is upregulated during the implantation window in both natural and hormone replacement therapy cycles in the endometrium. This upregulation, in the presence of a human blastocyst, leads to surface polarization of CXCR4 receptors, indicating its involvement in the adhesion phase of human implantation.
While SDF-1 and CXCR4 were once thought to form a relatively specific ligand-receptor pair, recent evidence suggests that ubiquitin is also a natural ligand for CXCR4. Chronic exposure to THC has been shown to increase CXCR4 expression on both CD4+ and CD8+ T lymphocytes. Additionally, drugs that block CXCR4 are capable of "mobilizing" hematopoietic stem cells into the bloodstream, facilitating the collection of peripheral blood stem cells.
Brief information
- Name: C-X-C motif chemokine receptor 4
- Target Synonym: NPYRL, CD184,CXCR4, CXC-R4,SDF-1 receptor, LAP-3,Fusin, FB22,HM89, Seven-Transmembrane-Segment Receptor, Spleen, Chemokine (C-X-C Motif), Receptor 4 (Fusin), Seven Transmembrane Helix Receptor, C-X-C Chemokine Receptor Type 4, Neuropeptide Y Receptor Y3, Neuropeptide Y3 Receptor, Chemokine Receptor, D2S201E,HSY3RR, NPYY3R, CXCR-4, NPY3R, WHIMS, LAP3, NPYR,WHIM, Receptors, CXCR4,LCR1, LESTR,LPS-associated protein 3, Leukocyte-Derived Seven Transmembrane Domain Receptor, Stromal Cell-Derived Factor 1 Receptor, Chemokine
- Number of Launched Drugs: 2
- Number of Drugs in Clinical Trials: 25
- Lastest Research Phase: Approved
Part of bioactivity data
CX4-H5219-MALS-HPLC. Image Credit: ACROBiosystems Inc.
Immobilized Human CXCR4 Full Length Protein-VLP (Cat. No. CX4-H5219) at a concentration of 5 μg/mL (100 μL per well) can bind Human ulocuplumab, Human IgG4, with a linear range of 1-31 ng/mL, as confirmed by QC testing.
Synonym name
- CXCR4, CD184, Fusin, D2S201E, FB22, HM89, HSY3RR, LAP3, LCR1, LESTR, NPY3R, NPYR, NPYRL, NPYY3R, WHIM