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  • An orally available human C-C chemokine receptor type 2 (CCR2) antagonist, with potential immunomodulating and antineoplastic activities. Upon oral administration, CCR2 antagonist CCX872-B specifically binds to CCR2 and prevents the binding to its cognate endothelium-derived chemokine ligand CCL2 (monocyte chemoattractant protein-1 or MCP1). This may result in the inhibition of both CCR2 activation and CCR2-mediated signal transduction, which may inhibit inflammatory processes, angiogenesis, tumor cell migration, and tumor cell proliferation. The G-protein coupled receptor CCR2 is expressed on the surface of monocytes and macrophages, and stimulates their migration and infiltration; it plays a key role in inflammation. CCR2 is overexpressed in certain cancer cell types, where it is involved in angiogenesis, tumor cell migration and proliferation. Check for \'https://www.cancer.gov/about-cancer/treatment/clinical-trials/intervention/C120302\' active clinical trials using this agent. (\'http://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI%20Thesaurus&code=C120302\' NCI Thesaurus)
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