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Mini-Reviews in Medicinal Chemistry


ISSN (Print): 1389-5575
ISSN (Online): 1875-5607

Review Article

An Overview of Bioactive Peptides for in vivo Imaging and Therapy in Human Diseases

Author(s): Anna Lucia Tornesello*, Maria Lina Tornesello and Franco M. Buonaguro

Volume 17 , Issue 9 , 2017

Page: [758 - 770] Pages: 13

DOI: 10.2174/1389557517666170120151739

Price: $65


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.

Keywords: Human cancer, non-oncologic diseases, nuclear medicine, radiolabeled peptides, radionuclides, radiopharmaceutical peptides, receptor targeting.

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