Preparation and SPECT imaging of the novel Anxa 1-targeted probe 99mTc-p-SCN-Bn-DTPA-GGGRDN-IF7

Abstract

Annexin 1 (Anxa1) is a highly specific surface marker of tumor vasculature in several solid tumors. The IF7 peptide was modified with a hydrophic linkers,GGGRDN, and introduced into a new bifunctional chelating agent p-SCN-Bn-DTPA. The resulting peptides (p-SCN-Bn-DTPA-GGGRDN-IF7) was successfuly labeled with 99mTc. The targeting characteristics to Anxa1 of the radiolabeled peptide were evaluated by in vitro and in vivo study is on U87 tumor models. SPECT imaging revealed that the U87 tumors were clearly visualized (3.64 ± 0.44%ID/g at 2 h p.i.). 99mTc-p-SCN-Bn-DTPA-GGGRDN-IF7 (Tc-RIF7) might be a potential target probe for detecting Anxa1 levels in cancers due to the favorable characterizations such as convenient synthesis, specific Anxa1 targeting and moderate tumor uptakes.