title: Synthesis of functionalised HP-DO3A chelating agents for conjugation to biomolecules.
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.(90)Y(iii), (177)Lu(iii) and (111)In(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 (111)In(iii) to obtain a new radiopharmaceutical product with potential applications in the diagnosis of tumors over-expressing oxytocin receptors.
authors.affiliation: Dipartimento di Scienza e Tecnologia del Farmaco, Università di Torino, Via Giuria 9, 10125 Torino, Italy.
authors.forename: Alessandro
authors.initials: A
authors.lastname: Barge
authors.forename: Enrico
authors.initials: E
authors.lastname: Cappelletti
authors.forename: Giancarlo
authors.initials: G
authors.lastname: Cravotto
authors.forename: Aurelia
authors.initials: A
authors.lastname: Ferrigato
authors.forename: Luciano
authors.initials: L
authors.lastname: Lattuada
authors.forename: Fabio
authors.initials: F
authors.lastname: Marinoni
authors.forename: Lorenzo
authors.initials: L
authors.lastname: Tei
mesh_terms: D002614:Chelating Agents / Q000138:chemical synthesis* / Q000737:chemistry*; D006573:Heterocyclic Compounds, 1-Ring / Q000138:chemical synthesis* / Q000737:chemistry*; D007205:Indium Radioisotopes / Q000737:chemistry; D007553:Isotope Labeling; D008024:Ligands; D010121:Oxytocin / Q000737:chemistry; D010455:Peptides / Q000737:chemistry
chemical_list: C544520:10-(2-hydroxypropyl)-1,4,7-tetraazacyclododecane-1,4,7-triacetic acid; D002614:Chelating Agents; D006573:Heterocyclic Compounds, 1-Ring; D007205:Indium Radioisotopes; D008024:Ligands; D010455:Peptides; D010121:Oxytocin