Preparation and biological evaluation of 99mTc-HYNIC-(Ser)3-D4 peptide for targeting and imaging of non-small-cell lung cancer.

Abstract

In this study, radiolabeled D4 peptide conjugate was studied as a radiotracer for imaging of non-small-cell lung cancer with overexpression of EGFR. HYNIC-(Ser)3-D4 peptide was labeled with 99mTc using tricine as a co-ligand. Cellular specific binding and internalization as well as in vivo tumor targeting were assessed. The in vitro experiments showed good cellular specific binding. Tumor uptake values as %ID/g were 7.55 and 6.82% at 1 and 4 h after injection, respectively. The presaturation of EGFR in xenografted nude mice reduced 36% tumor uptake of radioactivity at 1 h after injection that confirmed in vivo specificity. Findings showed this radiolabeled peptide is a promising candidate for tumor targeting and molecular imaging of non-small-cell lung cancer.