Tag: CXCR4

Balixafortide is a Selective and Well-Tolerated Peptidic CXCR4 Antagonist

Despite the introduction of new targeted therapies and cytotoxic agents, chemotherapy-pretreated metastatic breast cancer (MBC) remains an essentially incurable disease with only moderate median overall survival (OS). over 20 human tumor types overexpress C-X-C chemokine receptor type 4 (CXCR4). CXCR4 levels correlate with aggressive metastatic phenotypes and negative prognosis...

WZ811 is an Orally Active CXCR4 Antagonist

The C-X-C chemokine receptor-4 (CXCR4) is a seven-transmembrane G-protein coupled receptor (GPCR). It is a member of the family I GPCR or rhodopsin-like GPCR family. The chemokine stromal cell-derived factor-1 (SDF-1 or CXCL12) is a CXC chemokine peptide. Meanwhile, it is the natural ligand for CXCR4. Importantly, the CXCR4...

MSX-122, a Partial Antagonist of CXCR4, Has Anti-Metastasis Activity

In previous blog “MSX-122 is a Partial Antagonist of CXCR4”, I described MSX-122 as an orally available, specific small molecule antagonist of CXCR4/CXCL12. And it has good anti-inflammatory properties. However, MSX-122 entered into clinical trials tested among breast cancer patients. Accordingly, MSX-122 is a promising clinical candidate for cancer...