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Sentinel lymph node (SLN) imaging plays an important role in surgery of patients with breast cancer and melanoma. Therefore, radiopharmaceuticals that can specifically target mannose receptors on the surface of macrophages in LN are on strong demand for SLN imaging. In this study, we selected avidin for radiolabeling, because it is a tetrameric protein glycosylated with mannose and N-acetylglucosamine. We prepared ⁶⁴Cu-labeled avidin with and without conjugation of extra mannose molecules and evaluated them for PET/CT imaging of LN.

Mannose-conjugated avidin was prepared from avidin and α-D mannopyranosylphenyl isothiocyanate. Avidin and mannose-conjugated avidin were reacted with DOTA-NHS ester at room temperature for 22 h. The products were purified using PD-10 columns, lyophilized, and then analyzed by MALDI-TOF mass spectrometry. DOTA-conjugated …