In this review, we summarise the role of CXCR4 and CXCL12 in tumour growth, metastasis, angiogenesis, and cancer cell-microenvironment interaction. Furthermore, we discuss the potential benefits of targeting CXCR4 with specific inhibitors to disrupt CXCR4-dependent tumour-stroma interactions.

2024年9月5日 · Chemokine receptor 4 (CXCR4) is a subtype receptor protein of the GPCR family with a seven-transmembrane structure widely distributed in human tissues. CXCR4 is involved in diseases (e.g., HIV-1 infection), cancer proliferation and metastasis, inflammation signaling pathways, and leukemia, making it a promising drug target.

AMD3100 was shown to specifically antagonize CXCR4, and thus to block the entry of the T-lymphotropic HIV strains (6–8). AMD3100 appears to be a highly specific inhibitor of CXCR4 ( 9 ): it only blocks, as measured by the Ca ++ flux, the signal pathway from CXCR4 (Figure 1 B) and not that of any other receptor for either CXC- or C–C ...

The CXCR4 receptor upon binding its ligands triggers multiple signaling pathways that orchestrate cell migration, hematopoiesis and cell homing, and retention in the bone marrow. However, CXCR4 also directly controls cell proliferation of ...

2024年12月19日 · The new peptide CXCR4 inhibitor, R54 impaired CXCR4 activity reducing cell growth, migration and signalling in human ovarian cancer cells. Moreover, CXCL12 promoted epithelial to mesenchymal transition through VIMENTIN and …

2024年12月5日 · We identified a novel heptapeptide that fully replicates the pharmacological profile of the parent peptide on CXCR4, including its potency, selectivity, and antagonistic activity, while demonstrating enhanced stability in a reductive environment.

Recently, CXCR4 has been reported to play an important role in cell survival, proliferation, migration, as well as metastasis of several cancers including breast cancer. This review is mainly focused on the current knowledge of the oncogenic role …

CXCR4 is a chemokine receptor that mediates invasion and metastasis. CXCR4 expression is transcriptionally regulated in cancer cells and is associated with aggressive phenotypes of prostate cancer. Previously, we and others have shown that the ERG transcription factor regulates CXCR4 expression in prostate cancer cells.

Immunofluorescent imaging and flow cytometry were performed to examine the expression of CXCR4 in the EJ and EJ-M3 cell lines. A highly specific CXCR4 antagonist, AMD3100, was used to inhibit metastatic growth, as assessed by an in vitro invasion assay.

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