Title:An Overview of Bioactive Peptides for in vivo Imaging and Therapy in Human Diseases
Volume: 17
Issue: 9
Author(s): Anna Lucia Tornesello*, Maria Lina Tornesello and Franco M. Buonaguro
Affiliation:
- (CROM), Istituto Nazionale Tumori ,Italy
Keywords:
Human cancer, non-oncologic diseases, nuclear medicine, radiolabeled peptides, radionuclides, radiopharmaceutical
peptides, receptor targeting.
Abstract: Background: Radiolabeled peptides, designed to bind with high affinity receptors selectively
expressed on cell membranes of different human tissues, represent valuable tools for in vivo imaging
of several human diseases. Solid-phase peptide synthesis as well as availability of bifunctional
chelating agents and prosthetic groups allows the production and radiolabeling of several peptidebased
molecules which are useful to target specific receptors on different cancer types. Among them,
octreotide and other analogues of somatostatin, vasoactive intestinal peptide, CCK analogues, bombesin,
α-MSH analogues, neurotensin, exendin, RGD, substance P, conjugated to appropriate chelators,
such as DTPA, NOTA, DOTA or TETA, and radiolabeled with specific radionuclides, have already
been translated into the clinical practice with remarkable sensitivity and diagnostic accurateness.
Conclusion: This review recapitulates the current applications in clinical practice of radiolabeled peptides
with particular attention to those employed for diagnosis and therapy in oncologic as well as nononcologic
human diseases.
