MLchartDataset catalogue

CXCR4/E-selectin antagonist GMI-1359

Term · Oncology and biomedicine · MLC-T-ONC-012853

An antagonist of both the C-X-C chemokine receptor type 4 (CXCR4) and E-selectin (CD62E), with potential antineoplastic activity. Upon administration, CXCR4/E-selectin antagonist GMI-1359 binds to both CXCR4 and E-selectin expressed on endothelial cells. The binding to CXCR4 prevents the binding of stromal-cell derived factor-1 (SDF-1; CXCL12) to CXCR4 and inhibits CXCR4 activation, which may result in decreased proliferation and migration of CXCR4-expressing tumor cells. The binding to E-selectin expressed on endothelial cells prevents their interaction with E-selectin ligand-expressing cancer cells. This may prevent tumor cell activation, migration and metastasis. CXCR4, a chemokine receptor belonging to the G protein-coupled receptor (GPCR) family, plays an important role in chemotaxis and angiogenesis, and is upregulated in several tumor cell types. E-selectin is a cell adhesion molecule involved in cell rolling, signaling and chemotaxis. Its overexpression has been associated with tumor angiogenesis and metastasis in several cancers.

Table 1. Record
IdentifierMLC-T-ONC-012853
FieldOncology and biomedicine
ReferencesNational Cancer Institute Thesaurus (CC BY 4.0)
Record as JSON
{
  "id": "MLC-T-ONC-012853",
  "term": "CXCR4/E-selectin antagonist GMI-1359",
  "field": "Oncology and biomedicine",
  "definition": "An antagonist of both the C-X-C chemokine receptor type 4 (CXCR4) and E-selectin (CD62E), with potential antineoplastic activity. Upon administration, CXCR4/E-selectin antagonist GMI-1359 binds to both CXCR4 and E-selectin expressed on endothelial cells. The binding to CXCR4 prevents the binding of stromal-cell derived factor-1 (SDF-1; CXCL12) to CXCR4 and inhibits CXCR4 activation, which may result in decreased proliferation and migration of CXCR4-expressing tumor cells. The binding to E-selectin expressed on endothelial cells prevents their interaction with E-selectin ligand-expressing cancer cells. This may prevent tumor cell activation, migration and metastasis. CXCR4, a chemokine receptor belonging to the G protein-coupled receptor (GPCR) family, plays an important role in chemotaxis and angiogenesis, and is upregulated in several tumor cell types. E-selectin is a cell adhesion molecule involved in cell rolling, signaling and chemotaxis. Its overexpression has been associated with tumor angiogenesis and metastasis in several cancers.",
  "references": [
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/cxcr4-e-selectin-antagonist-gmi-1359/"
}

Record 5,550 of 17,717 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.