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 90Y-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.

A New Biotin Derivative-DOTA Conjugate as a Candidate for Pre-targeted Diagnosis and Therapy of Tumors / G. SABATINO; M. CHINOL; G. PAGANELLI; S. PAPI; M. CHELLI; G. LEONE; A.M. PAPINI; A. DE LUCA; M. GINANNESCHI. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - STAMPA. - 46:(2003), pp. 3170-3173. [10.1021/jm030789z]

A New Biotin Derivative-DOTA Conjugate as a Candidate for Pre-targeted Diagnosis and Therapy of Tumors.

SABATINO, GIUSEPPINA;LEONE, GIUSEPPE;PAPINI, ANNA MARIA;M. GINANNESCHI
2003

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 90Y-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.
2003
46
3170
3173
G. SABATINO; M. CHINOL; G. PAGANELLI; S. PAPI; M. CHELLI; G. LEONE; A.M. PAPINI; A. DE LUCA; M. GINANNESCHI
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Utilizza questo identificatore per citare o creare un link a questa risorsa: https://hdl.handle.net/2158/219599
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