99mTc-HYNIC-(Ser)3-J18 peptide: A radiotracer for non-small-cell lung cancer targeting

Abstract

Radiolabeled peptide could be a useful tool for the diagnosis of non-small-cell lung cancer (NSCLC). In this study, HYNIC-(Ser)₃-J18 peptide was labeled with ^99mTc using EDDA/tricine as co-ligands. The in vitro and in vivo studies of this radiolabeled peptide were performed for cellular specific binding and tumor targeting in A-549 cells and tumor bearing mice, respectively. The high radiochemical purity was obtained and this radiolabeled peptide exhibited high stability in buffer and serum. The radiolabeled peptide showed high affinity for the A-549 cells with a dissociation constant value (K_D) of 4.4 ± 0.8 nM. The tumor-muscles ratios were 2.7 and 4.4 at 1 and 2 h after injection of ^99mTc-(EDDA/tricine)-HYNIC-(Ser)₃-J18 in tumor bearing mice. The tumor uptake was decreased after pre-injection with non-labeled peptide for this radiolabeled peptide in blocking experiment. The results of this study showed the ^99mTc-(EDDA/tricine)-(Ser)₃-HYNIC-J18 peptide might be a promising radiolabeled peptide for NSCLC targeting.

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This study described the preparation and radiolabeling of HYNIC-J18 peptide with ^99mTc and EDDA/tricine as co-ligand. The ^99mTc-J18 peptide was evaluated for specific binding to non-small cell lung cancer. Results of this study showed that ^99mTc-(EDDA/tricine)-(Ser)₃-HYNIC-J18 peptide might be a promising radiolabeled peptide for NSCLC targeting.

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