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

Publisher: Bentham Science Publishers

E-ISSN: 1875-5607|17|9|758-770

ISSN: 1389-5575

Source: Mini Reviews in Medicinal Chemistry, Vol.17, Iss.9, 2017-05, pp. : 758-770

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Abstract

Background: Radiolabeled peptides, designed to bind with high affinity receptors selectivelyexpressed on cell membranes of different human tissues, represent valuable tools for in vivo imagingof several human diseases. Solid-phase peptide synthesis as well as availability of bifunctionalchelating agents and prosthetic groups allows the production and radiolabeling of several peptidebasedmolecules 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,?-MSH analogues, neurotensin, exendin, RGD, substance P, conjugated to appropriate chelators,such as DTPA, NOTA, DOTA or TETA, and radiolabeled with specific radionuclides, have alreadybeen translated into the clinical practice with remarkable sensitivity and diagnostic accurateness.Conclusion: This review recapitulates the current applications in clinical practice of radiolabeled peptideswith particular attention to those employed for diagnosis and therapy in oncologic as well as nononcologichuman diseases.