Two novel bifunctional chelating agents (BFCAs) based on the structure of 10-(2-hydroxypropyl)1,4,7-tetraazacyclododecane-1,4,7-triacetic acid (HP-DO3A) have been designed and synthesized. BFCAs are able to strongly coordinate metals (e. g. Gd(III)) and radiometals (e. g. Y-90(III), Lu-177(III) and In-111(III)), and find applications in the synthesis of products for the imaging and treatment of several cancer types. Indeed, these two BFCAs have been employed in solid-phase peptide synthesis (SPPS) and coupled to well-known peptides such as bombesin and RGD analogues in order to target tumor cells. We also report here the conjugation of one of them to Lys(8)-oxytocin and radiolabeling with In-111(III) to obtain a new radiopharmaceutical product with potential applications in the diagnosis of tumors over-expressing oxytocin receptors.

Synthesis of functionalised HP-DO3A chelating agents for conjugation to biomolecules

BARGE, Alessandro;CRAVOTTO, Giancarlo;
2009-01-01

Abstract

Two novel bifunctional chelating agents (BFCAs) based on the structure of 10-(2-hydroxypropyl)1,4,7-tetraazacyclododecane-1,4,7-triacetic acid (HP-DO3A) have been designed and synthesized. BFCAs are able to strongly coordinate metals (e. g. Gd(III)) and radiometals (e. g. Y-90(III), Lu-177(III) and In-111(III)), and find applications in the synthesis of products for the imaging and treatment of several cancer types. Indeed, these two BFCAs have been employed in solid-phase peptide synthesis (SPPS) and coupled to well-known peptides such as bombesin and RGD analogues in order to target tumor cells. We also report here the conjugation of one of them to Lys(8)-oxytocin and radiolabeling with In-111(III) to obtain a new radiopharmaceutical product with potential applications in the diagnosis of tumors over-expressing oxytocin receptors.
2009
7
3810
3816
mri contrast agent; bifunctional chelators; radiolabeled peptides; convenient synthesis; dota derivatives; therapy; chemistry; radiopharmaceuticals; gadolinium(iii); radiotherapy
Barge A.; Cappelletti E.; Cravotto G.; Ferrigato A.; Lattuada L.; Marinoni F.; Tei l.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2318/62996
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