CXC趋化因子受体4(CXCR4)是最主要的趋化因子受体之一,在多种类型细胞中均有表达,包括淋巴细胞、造血干细胞、内皮细胞和肿瘤细胞。CXCR4与其配体——基质细胞衍生因子1(SDF-1)(也称CXCL12)结合,能介导多种与细胞趋化、细胞存活或增殖相关信号传导通路。CXCR4与SDF-1轴涉及肿瘤的恶性演进、血管生成、转移和存活。因此,阻断CXCR4与SDF-1轴及下游信号通路成为相关治疗的分子靶标。
CXCR4, one of the most important chemokine receptor in tumor, is expressed in multiple cell types including lymphocytes, hematopoietic stem cells, endothelial and epithelial cells, and cancer cells. The binding of CXCR4 to its ligand CXCL12 [stromal cell-derived factor-1 (SDF-1)] induces intracellular signaling through several divergent pathways initiating signals related to chemotaxis, cell survival and/or proliferation. SDF-1/CXCR4 axis is involved in tumor progression, angiogenesis, metastasis, and survival. Therefore, this pathway is a target for therapeutics that can block the CXCL12/CXCR4 interaction or inhibit downstream intracellular signaling.