title: Chelating systems for (99m)Tc/(188)Re in the development of radiolabeled peptide pharmaceuticals.
abstract: Currently, receptor based radiopharmaceuticals have received great attention in molecular imaging and radiotherapy of cancer, and provide a unique tool for target-specific delivery of radionuclides to pathological tissues. In this context, receptor binding peptides represent an attractive class of target vectors for Nuclear Medicine purposes. The rich chemistry of the group 7 elements elaborated in past years, has allowed the development of different procedures for the preparation of radiolabeled peptides in high yield. This, joint to the use of solid-phase peptide synthesis, has opened the possibility to explore new strategies for approaching the design of new class of radiolabeled receptor-targeted peptides, and to create new versatilities in targeting vehicle design e.g. in synthesis of metal-cyclized peptides or of multivalent targeting agents. This review provides an overview on several aspects of the development of new (99m)Tc/(188)Re-peptide based target specific radiopharmaceuticals, in particular on the synthetic strategies employed for modifying molecular vectors, and the application of the different metal-cores and/or building block for preparing high specific activity agents.
authors.affiliation: ICIS-CNR, Corso Stati Uniti, 4, 35127 Padova, Italy. refosco@icis.cnr.it
authors.forename: Cristina
authors.initials: C
authors.lastname: Bolzati
authors.forename: Davide
authors.initials: D
authors.lastname: Carta
authors.forename: Nicola
authors.initials: N
authors.lastname: Salvarese
authors.forename: Fiorenzo
authors.initials: F
authors.lastname: Refosco
mesh_terms: D000595:Amino Acid Sequence; D000818:Animals; D002614:Chelating Agents / Q000737:chemistry / Q000627:therapeutic use; D006801:Humans; D008958:Models, Molecular; D008969:Molecular Sequence Data; D009369:Neoplasms / Q000175:diagnosis* / Q000378:metabolism / Q000532:radiotherapy*; D010455:Peptides / Q000737:chemistry* / Q000627:therapeutic use; D019275:Radiopharmaceuticals / Q000737:chemistry* / Q000627:therapeutic use; D018000:Receptors, Peptide / Q000378:metabolism; D012211:Rhenium / Q000737:chemistry* / Q000627:therapeutic use; D060327:Solid-Phase Synthesis Techniques; D013667:Technetium / Q000737:chemistry* / Q000627:therapeutic use
chemical_list: D002614:Chelating Agents; D010455:Peptides; D019275:Radiopharmaceuticals; D018000:Receptors, Peptide; D012211:Rhenium; D013667:Technetium