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Synthetic procedures for 111In-labeled Fabs used in this study. An FGK sequence was selected as a cleavable linkage to liberate the Phe adduct of the chelators as the radiometabolites. The arrows show the peptide bond expected to be cleaved by ACE. While [111In]In-DOTA-Bn forms a net negative charged (−1) complex, [111In]In-DO3AiBu-Bn provides a neutral complex with a lipophilic isobutyl group. [111In]In-DOTA-Bn-FGK-Fab was prepared by the conventional method and used as a reference.
