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Tc‐99m Glu‐Cys‐Gly‐His‐Gly‐Lys (ECG‐HGK), a novel Tc‐99m labeled hexapeptide for molecular tumor imaging
Author(s) -
Kim DaeWeung,
Kim Myoung Hyoun,
Kim Chang Guhn
Publication year - 2016
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.3378
Subject(s) - chemistry , in vivo , thioester , peptide , biodistribution , in vitro , biochemistry , stereochemistry , enzyme , microbiology and biotechnology , biology
Domain 5 of kinin‐free high molecular weight kininogen inhibits the adhesion of many tumor cell lines, and it has been reported that the histidine–glycine–lysine (HGK)‐rich region might be responsible for inhibition of cell adhesion. The authors developed HGK‐containing hexapeptide, glutamic acid–cysteine–glycine (ECG)–HGK, and evaluated the utility of Tc‐99m ECG‐HGK for tumor imaging. Hexapeptide, ECG‐HGK was synthesized using Fmoc solid‐phase peptide synthesis. Radiolabeling efficiency was evaluated. The uptake of Tc‐99m ECG‐HGK within HT‐1080 cells was evaluated in vitro . In HT‐1080 tumor‐bearing mice, gamma imaging and biodistribution studies were performed. The complexes Tc‐99m ECG‐HGK was prepared in high yield. The uptake of Tc‐99m ECG‐HGK within the HT‐1080 tumor cells had been demonstrated by in vitro studies. The gamma camera imaging in the murine model showed that Tc‐99m ECG‐HGK was accumulated substantially in the HT‐1080 tumor (tumor‐to‐muscle ratio = 5.7 ± 1.4 at 4 h), and the tumoral uptake was blocked by the co‐injection of excess HGK (tumor‐to‐muscle ratio = 2.8 ± 0.6 at 4 h). In the present study, Tc‐99m ECG‐HGK was developed as a new tumor imaging agents. Our in vitro and in vivo studies revealed specific function of Tc‐99m ECG‐HGK for tumor imaging.