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Molecules 2017, 22(8), 1282; doi:10.3390/molecules22081282

New Insights in the Design of Bioactive Peptides and Chelating Agents for Imaging and Therapy in Oncology

Molecular Biology and Viral Oncology Unit, Istituto Nazionale Tumori, IRCCS, Fondazione Pascale, 80131 Napoli, Italy
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Received: 30 May 2017 / Accepted: 25 July 2017 / Published: 2 August 2017
(This article belongs to the Special Issue Peptide-Based Drugs and Drug Delivery Systems)
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Abstract

Many synthetic peptides have been developed for diagnosis and therapy of human cancers based on their ability to target specific receptors on cancer cell surface or to penetrate the cell membrane. Chemical modifications of amino acid chains have significantly improved the biological activity, the stability and efficacy of peptide analogues currently employed as anticancer drugs or as molecular imaging tracers. The stability of somatostatin, integrins and bombesin analogues in the human body have been significantly increased by cyclization and/or insertion of non-natural amino acids in the peptide sequences. Moreover, the overall pharmacokinetic properties of such analogues and others (including cholecystokinin, vasoactive intestinal peptide and neurotensin analogues) have been improved by PEGylation and glycosylation. Furthermore, conjugation of those peptide analogues to new linkers and bifunctional chelators (such as AAZTA, TETA, TRAP, NOPO etc.), produced radiolabeled moieties with increased half life and higher binding affinity to the cognate receptors. This review describes the most important and recent chemical modifications introduced in the amino acid sequences as well as linkers and new bifunctional chelators which have significantly improved the specificity and sensitivity of peptides used in oncologic diagnosis and therapy. View Full-Text
Keywords: peptide; chemical modification; peptide cyclization; d-amino acids; glycosylation; PEGylation; chelators; TETA; AAZTA; DOTA; TRAP; NOPO peptide; chemical modification; peptide cyclization; d-amino acids; glycosylation; PEGylation; chelators; TETA; AAZTA; DOTA; TRAP; NOPO
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Tornesello, A.L.; Buonaguro, L.; Tornesello, M.L.; Buonaguro, F.M. New Insights in the Design of Bioactive Peptides and Chelating Agents for Imaging and Therapy in Oncology. Molecules 2017, 22, 1282.

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