NCIt definition : An orally available human chemokine receptor 2 (CCR2) antagonist with potential immunomodulating
and antineoplastic activities. Upon oral administration, CCR2 antagonist PF-04136309
specifically binds to CCR2 and prevents binding of the endothelium-derived chemokine
ligand CLL2 (monocyte chemoattractant protein-1 or MCP1) to its receptor CCR2, which
may result in inhibition of CCR2 activation and signal transduction. This may inhibit
inflammatory processes as well as angiogenesis, tumor cell migration, and tumor cell
proliferation. The G-protein coupled receptor CCR2 is expressed on the surface of
monocytes and macrophages, stimulates the migration and infiltration of these cell
types, and plays an important role in inflammation, angiogenesis, and tumor cell migration
and proliferation.;
Semantic type(s)