A new biotin derivative-DOTA conjugate as a candidate for pretargeted diagnosis and therapy of tumors.
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.
Sabatino
Giuseppina
G
Department of Organic Chemistry "Ugo Schiff", University of Florence, and CNR-ICCOM, Polo Scientifico, Via della Lastruccia 13, I-50019 Sesto Fiorentino (FI), Italy.
Chinol
Marco
M
Paganelli
Giovanni
G
Papi
Stefano
S
Chelli
Mario
M
Leone
Giuseppe
G
Papini
Anna Maria
AM
De Luca
Angelo
A
Ginanneschi
Mauro
M
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
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