Stromal cell-derived factor 1 receptor (CXCR4) (CXCR4)

CXCR4 is a G protein-coupled chemokine receptor that binds stromal cell-derived factor 1 (SDF-1, also known as CXCL12). This receptor–ligand pair plays a critical role in chemotaxis, particularly in the homing and migration of hematopoietic stem and progenitor cells, as well as in neuronal development, angiogenesis, immune regulation, and tissue repair[2][6][7][8]. CXCR4 is widely expressed on hematopoietic, endothelial, epithelial, neural, and cancer cells. The SDF-1/CXCR4 axis is a well-established therapeutic target—especially in cancer (mediating tumor progression, metastasis, and angiogenesis), HIV infection (as a viral co-receptor), and stem cell mobilization[5][6]. Drugs antagonizing CXCR4, such as plerixafor, are approved for stem cell mobilization in transplantation. Pathological activation or inhibition of this axis is associated with a range of clinical conditions, highlighting its importance as a biomarker and a target for therapy. Note: The phrase "SDF-1/CXCL12 interaction with CXCR4" describes the ligand–receptor interaction, but the canonical therapeutic target is the receptor (CXCR4). SDF-1 (CXCL12) alone is a chemokine, not typically itself a direct drug target, although it is measured as a biomarker or blocked as part of the ligand–receptor axis. References: Summarized and synthesized from [1][2][3][4][5][6][7][8].

Other names

C-X-C chemokine receptor type 4CD184Chemokine (C-X-C motif) receptor 4SDF-1 receptorFusin

CXCR4 antagonism (blocks SDF-1/CXCL12 binding) - Inhibiting chemotaxis and migration - Mobilization of hematopoietic stem cells - Interrupts cancer cell homing/metastasis - Inhibition of viral entry (HIV co-receptor blockade)