Chemokine (C-X-C motif) receptor 4 (CXCR4), a chemokine receptor expressed by immune and tumor cells, guides tumor-cell migration and is important for processes such as tumor metastasis. Inhibition of CXCR4 may impair these protumor effects.
- CXCR4 is a G-protein–coupled receptor in the CXC chemokine receptor family found on the surface of immune cells, such as T cells1-3
- The ligand for CXCR4 is (chemokine (C-X-C motif) ligand 12) CXCL12 or stromal
cell-derivedfactor 1 (SDF-1), which is expressed by cells such as osteoblasts and endothelial cells5
- Binding of CXCR4 to its ligand CXCL12 directs the migration and recruitment of immune cells,5,6 and is implicated in several biological processes such as immune response and cardiovascular development5
- Preclinical data suggest that inhibition of the CXCR4 pathway may have a dual effect, as it impairs tumor-cell migration and blocks tumor growth.10 It also increases mobilization of leukocytes and leukemic blasts into the peripheral circulation, resulting in significant antileukemic activity11
1. Xu C, Zhao H, Chen H, Yao Q. CXCR4 in breast cancer: oncogenic role and therapeutic targeting. Drug Des Devel Ther.