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Gastrin-releasing peptide receptors (GRPRs) expressed on human tumors can serve as molecular targets for radiolabeled peptide analogs based on the frog tetradecapeptide bombesin (BBN). We have recently expanded this approach toward human GRP(18-27) sequences and introduced (99m)Tc-demomedin C, our first radiotracer based on GRP(18-27), showing favorable biologic characteristics during preclinical evaluation in rodents. We now present a series of (99m)Tc-demomedin C analogs, generated by single-Gly(24) or double-Gly(24)/Met(27) substitutions in the peptide chain, and compare their performance in GRPR-positive in vitro and in vivo models.

99mTc Radiotracers Based on Human GRP(18-27): Synthesis and Comparative Evaluation

^99mTc Radiotracers Based on Human GRP(18-27): Synthesis and Comparative Evaluation