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

Alessandro Barge, Enrico Cappelletti, Giancarlo Cravotto, Aurelia Ferrigato, Luciano Lattuada, Fabio Marinoni, Lorenzo Tei

Risultato della ricerca: Contributo su rivistaArticolo in rivistapeer review

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.90Y(iii), 177Lu(iii) and 111In(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 111In(iii) to obtain a new radiopharmaceutical product with potential applications in the diagnosis of tumors over-expressing oxytocin receptors.

Lingua originaleInglese
pagine (da-a)3810-3816
Numero di pagine7
RivistaOrganic and Biomolecular Chemistry
Volume7
Numero di pubblicazione18
DOI
Stato di pubblicazionePubblicato - 2009

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