C-X-C chemokine receptor 4 (CXCR4) is a receptor for the stromal cell-derived factor-1 (SDF-1) which is designated as chemokine ligand 12 (CXCL12). It is involved in cell progression, hematopoiesis, cancer, HIV entry, and rheumatoid arthritis.^1,2,3 FC 131 is an inhibitor of CXCR4 activation by SDF-1 (IC₅₀ = 4.5 nM) and also blocks HIV-induced cytopathogenicity (EC₅₀ = 73 nM).³ FC 131 derivatives can be used for imaging CXCR4 and elucidating its function.⁴

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1.Broxmeyer, H.E.,Orschell, C.M.,Clapp, D.W., et al. Rapid mobilization of murine and human hematopoietic stem and progenitor cells with AMD3100, a CXCR4 antagonist. Journal of Experimental Medicine 201(8), 1307-1318 (2005).

2.Dorsam, R.T. and Gutkind, J.S. G-protein-coupled receptors and cancer. Nature Reviews.Cancer 7, 79-94 (2007).

3.Tamamura, H.,Hiramatsu, K.,Ueda, S., et al. Stereoselective synthesis of [L-Arg-L/D-3-(2-naphthyl)alanine]-type (E)-alkene dipeptide isosteres and its application to the synthesis and biological evaluation of pseudopeptide analogues of the CXCR4 antagonist FC131. Journal of Medicinal Chemistry 48, 380-391 (2005).

4.Kuil, J.,Buckle, T. and van Leeuwen, F.W.B. Imaging agents for the chemokine receptor 4 (CXCR4). Chem.Soc.Rev. 41, 5239-5261 (2012).