title: A new biotin derivative-DOTA conjugate as a candidate for pretargeted diagnosis and therapy of tumors.
abstract: The synthesis of a new biotin derivative, the (CO) reduced N-aminohexyl biotinamido derivative, designed to be serum biotinidase resistant, and its conjugation to the chelator DOTA through an amide bond at one of the four carboxymethyl chains are described. The (90)Y-labeled conjugate was able to bind avidin at different Av/conjugate molar ratios with good results. The preclinical results indicate that this new biotin-DOTA conjugate is a good candidate for pretargeted diagnosis and therapy of tumors.
authors.affiliation: Department of Organic Chemistry "Ugo Schiff", University of Florence, and CNR-ICCOM, Polo Scientifico, Via della Lastruccia 13, I-50019 Sesto Fiorentino (FI), Italy.
authors.forename: Giuseppina
authors.initials: G
authors.lastname: Sabatino
authors.forename: Marco
authors.initials: M
authors.lastname: Chinol
authors.forename: Giovanni
authors.initials: G
authors.lastname: Paganelli
authors.forename: Stefano
authors.initials: S
authors.lastname: Papi
authors.forename: Mario
authors.initials: M
authors.lastname: Chelli
authors.forename: Giuseppe
authors.initials: G
authors.lastname: Leone
authors.forename: Anna Maria
authors.initials: AM
authors.lastname: Papini
authors.forename: Angelo
authors.initials: A
authors.lastname: De Luca
authors.forename: Mauro
authors.initials: M
authors.lastname: Ginanneschi
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry; D001360:Avidin / Q000737:chemistry; D001710:Biotin / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000737:chemistry; D002614:Chelating Agents / Q000138:chemical synthesis / Q000737:chemistry; D004355:Drug Stability; D006573:Heterocyclic Compounds, 1-Ring / Q000138:chemical synthesis* / Q000737:chemistry; D006801:Humans; D007553:Isotope Labeling; D009369:Neoplasms / Q000175:diagnosis; D011485:Protein Binding; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000737:chemistry; D015019:Yttrium
chemical_list: D000970:Antineoplastic Agents; D002614:Chelating Agents; D006573:Heterocyclic Compounds, 1-Ring; D019275:Radiopharmaceuticals; D001360:Avidin; C071349:1,4,7,10-tetraazacyclododecane- 1,4,7,10-tetraacetic acid; D015019:Yttrium; D001710:Biotin