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Report No.

Synthesis and ${it in vitro}$ Evaluation of $$^{64}$$Cu-labeled peptide for tumor imaging

Sugo, Yumi; Sasaki, Ichiro; Watanabe, Shigeki; Ohshima, Yasuhiro; Ishioka, Noriko

HER2 is a member of the epidermal growth factor receptor family, which is overexpressed on the surface of tumor cells. H-Met-Ala-Arg-Ser-Gly-Leu-OH (MARSGL) is a linear peptide having high affinity to HER2 overexpressing in various cancer cells. In the previous study, we have synthesized a novel radioiodinated MARSGL via electrophilic destannylation in high radiochemical yield. $$^{64}$$Cu is an attractive radionuclide for positron emission tomography imaging as well as radiotherapy due to its half-life of 12.7 h and decay characteristics of both $$beta$$$$^{+}$$ and $$beta$$$$^{-}$$. 1,4,7,10-Tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) is a macrocyclic ligand for various metal ions. In this study, we designed and synthesized $$^{64}$$Cu-labeled MARSGL peptide conjugated with DOTA as an imaging probe for HER2 overexpressing tumors. In order to evaluate the usefulness of $$^{64}$$Cu-DOTA-MARSGL peptide as a PET imaging probe,${it in vitro}$ studies were also performed.



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