Design of Peptide Imaging Agents for Whole-body and Intraoperative Molecular Imaging

Abstract

Due to the growing toolkit of targeted contrast agents, molecular imaging continues to play a prominent role in the clinical care of cancer. Peptide-based imaging approaches are of particular significance due to their favorable pharmacokinetic properties, established manufacturing infrastructure, and documented clinical success in whole-body imaging. A logical extension of molecular imaging with peptides is to improve surgical outcomes in cancer through highly sensitive and specific probes which can be used intraoperatively. Advances in fluorescent imaging have resulted in various peptide labeling strategies with intraoperative indications. In this review, we focused on the evolving design of peptide imaging agents starting with the clinically used somatostatin targeting peptides. We then review the current synthetic approaches used for dual-labeled agent development and offer perspectives on optimal protection schemes that can be used for multimodal probe development.

Peptide‐Decorated Dendrimers and Their Bioapplications

“…Important imaging modalities applied to PDDs include radionuclide‐based imaging and fluorescence‐based optical imaging where many peptide ligands have been functionalized with radioactive and/or fluorescent labels to attain receptor imaging . However, care must be taken as labeling peptides often causes a drop in peptide binding and function and may also alter their biodistribution .…”

Peptides for diagnosis and treatment of ovarian cancer

“…In addition to radiolabeling, optical imaging of fluorescently labeled peptides may be advantageous because it may improve the detection of metastatic tumor deposits while reducing the risk of population radioactivity exposure (42,43). Liu and colleagues (34) report the biological characterization of fluorescently labeled GE137 (c-Met targeting peptide) in ovarian cancer cells.…”

Mit Peptiden dekorierte Dendrimere und ihre biotechnologische Nutzung

“…Wichtige bildgebende Verfahren mit PDDs sind die Radionuclid‐ und die Fluoreszenz‐basierte optische Bildgebung; zu diesem Zweck wurden zahlreiche Peptidliganden mit radioaktiven und/oder Fluoreszenzmarkern funktionalisiert, um Rezeptoren abzubilden . Bei der Markierung von Peptiden ist jedoch Vorsicht geboten, da das Peptid hierdurch häufig schlechter bindet, seine Funktion ändert und eine andere Verteilung im biologischen System aufweist .…”