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.
| Identifier | MLC-T-ONC-012853 |
|---|---|
| Field | Oncology and biomedicine |
| References | National 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.