In vivo and in vitro characterization of CCK8 bearing a histidine-based chelator labeled with 99mTc-tricarbonyl (Articolo in rivista)

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  • In vivo and in vitro characterization of CCK8 bearing a histidine-based chelator labeled with 99mTc-tricarbonyl (Articolo in rivista) (literal)
Anno
  • 2008-01-01T00:00:00+01:00 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#doi
  • 10.1002/bip.21041 (literal)
Alternative label
  • D'Andrea L.D., Testa I., Panico M., Di Stasi R., Caracò C., Tarallo L., Arra C., Barbieri A., Romanelli A., Aloj L (2008)
    In vivo and in vitro characterization of CCK8 bearing a histidine-based chelator labeled with 99mTc-tricarbonyl
    in Biopolymers (Print)
    (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#autori
  • D'Andrea L.D., Testa I., Panico M., Di Stasi R., Caracò C., Tarallo L., Arra C., Barbieri A., Romanelli A., Aloj L (literal)
Pagina inizio
  • 707 (literal)
Pagina fine
  • 712 (literal)
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  • 90 (literal)
Rivista
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#note
  • Pubblicazione su rivista internazionale (literal)
Note
  • ISI Web of Science (WOS) (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#affiliazioni
  • D'Andrea L.D., CNR, Ist Biostrutture & Bioimmagini, I-80134 Naples, Italy Testa I., CNR, Ist Biostrutture & Bioimmagini, I-80134 Naples, Italy Panico M., CNR, Ist Biostrutture & Bioimmagini, I-80134 Naples, Italy Di Stasi R., CNR, Ist Biostrutture & Bioimmagini, I-80134 Naples, Italy Caracò C., Fdn G Pascale, Ist Nazl Tumori, Area Funz Med Nucl, I-80131 Naples, Italy Tarallo L., Fdn G Pascale, Ist Nazl Tumori, Area Funz Med Nucl, I-80131 Naples, Italy Arra C., Fdn G Pascale, Ist Nazl Tumori, UOS Sperimentaz Anim, I-80131 Naples, Italy Barbieri A., Fdn G Pascale, Ist Nazl Tumori, UOS Sperimentaz Anim, I-80131 Naples, Italy Romanelli A., Univ Naples Federico 2, Dipartimento Sci Biol, I-80134 Naples, Italy Aloj L, Fdn G Pascale, Ist Nazl Tumori, Area Funz Med Nucl, I-80131 Naples, Italy (literal)
Titolo
  • In vivo and in vitro characterization of CCK8 bearing a histidine-based chelator labeled with 99mTc-tricarbonyl (literal)
Abstract
  • The development of receptor targeting radiolabeled ligands has gained much interest in recent years for diagnostic and therapeutic applications in nuclear medicine. Cholecystokinin (CCK) receptors have been shown to be overexpressed in a subset of neuroendocrine and other tumors. We are evaluating binding and biodistribution properties of a CCK8 peptide derivative labeled with Tc-99m(I)-tricarbonyl. The CCK8 peptide was modified at its N-terminus by adding to its N-terminus two lysine-histidine modules (KH), where histidine is coupled to the side chain of the lysine ((KH)(2)-CCK8). Tc-99m(I)-tricarbonyl was generated with the IsoLink (TM) kit. A431 cells stably transfected with a cDNA encoding for the human CCK2 receptor were utilized to determine binding affinity, internalization, and retention of the labeled peptide, in comparison with wild-type A431 cells. A nude mouse tumor model was obtained by generating A431-CCK2R and A431-control tumors in opposite flanks of the animals. High specific activity labeling with 99(m)Tc was achieved. In A431-CCK2R cells, specific saturable binding was observed as well as evident internalization of the radiolabeled peptide after binding. Biodistribution experiments showed rapid, specific localization of (KH)(2)-CCK8 on A431-CCK2R xenografts compared with control tun-tors, although absolute uptake values were not markedly higher compared with background activity. Clearance of unbound radioactivity was both urinary and hepatobiliary. In imaging experiments, while targeting to CCK2R positive tumors could be appreciated, there was poor contrast between target and nontarget areas. (KH)2-CCK8 shows adequate in vitro and in vivo properties for CCK2R targeting although improvement of biodistribution warrant further development. (literal)
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