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Target intelligence / Profile preview
C-X-C chemokine receptor type 4 (CXCR4)
- Target
- CXCR4
- Molecular classification
- G protein-coupled receptor, Chemokine receptor
01
Overview
C-X-C chemokine receptor type 4 (CXCR4) is a seven-transmembrane G protein-coupled receptor that binds the chemokine CXCL12 (stromal cell-derived factor 1, SDF-1). CXCR4 is expressed on hematopoietic stem cells and mediates their homing, retention, and recruitment to bone marrow and injured tissues. The CXCL12–CXCR4 axis is pivotal for HSC trafficking under both homeostatic and injury conditions. Pharmacological antagonism of CXCR4, notably with AMD3100 (Plerixafor), is used clinically to induce HSC mobilization for transplantation. CXCR4 signaling also plays roles in immunology, infection susceptibility, cancer biology, and tissue regeneration. CXCR4 is a prototypic chemokine receptor and its modulation constitutes a key strategy for therapeutic mobilization and recruitment of HSCs[1][5][7].
- Other names
- CXCR4FusinCD184CXC chemokine receptor 4SDF-1 receptor
02
Mechanism of action
CXCR4 antagonists block the interaction with CXCL12, mobilizing HSCs from bone marrow to peripheral circulation\nModulation of chemokine receptor signaling
03
Biological functions
Signal transductionCell migrationStem cell traffickingImmune responseCell retention in bone marrow niches
04
Disease associations
Cancer (hematologic malignancies, metastasis)Cardiovascular disease (following myocardial infarction)InflammationInfection (notably HIV entry via CXCR4)Other (tissue regeneration following injury)
05
Safety considerations
Over-mobilization can lead to cytopenias or undesirable redistribution of stem cellsPotential off-target effects, immunosuppression, or altered tissue repairCXCR4 antagonists can theoretically affect HIV susceptibility (as CXCR4 serves as a co-receptor for certain HIV strains)
06
Interacting drugs
AMD3100 (Plerixafor): CXCR4 antagonist used to mobilize HSCs
1 more in the full profile.
07
Biomarkers
CXCR4 expression (for patient selection in HSC mobilization)Circulating CD34+ cell count (for monitoring efficacy)
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