An inhibitor of αvβ3 integrin
Cyclo(RGDfK) is a synthetic lipopeptide inhibitor of αvβ3 integrin (IC50 = 1.33 nM).1 Osteoblast cultures, which express αvβ5 and αvβ3 integrins, but not M21L cells that do not express these integrins, bind to cyclo(RGDfK)-coated surfaces. Cyclo(RGDfK) is taken up into tumors in vivo and in vitro and it has been polymerized or conjugated to various fluorophores, radiolabels, and peptide sequences for use in fluorescent and PET imaging to study tumor cell adhesion.2,3,1
1.?ime?ek, J., Notni, J., Kapp, T.G., et al.Benefits of NOPO as chelator in gallium-68 peptides, exemplified by preclinical characterization of 68Ga-NOPO-c(RGDfK)Mol. Pharm.11(5)1687-1695(2014) 2.Dijkgraaf, I., Beer, A.J., and Wester, H.-J.Application of RGD-containing peptides as imaging probes for alphavbeta3 expressionFront. Biosci. (Landmark Ed.)14(3)887-899(2009) 3.Janssen, M., Oyen, W.J.G., Massuger, L.F.A.G., et al.Comparison of a monomeric and dimeric radiolabeled RGD-peptide for tumor targetingCancer Biother. Radiopharm.17(6)641-646(2002)
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