Preferred Label : CXCR4/E-selectin Antagonist GMI-1359;
NCIt 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.;
Molecule name : GMI-1359; GMI 1359;
NCI Metathesaurus CUI : CL972258;
Origin ID : C167271;
UMLS CUI : C5238416;
Semantic type(s)
- concept_is_in_subset
- has_target
