New macrobicyclic chelator for the development of ultrastable 64Cu-radiolabeled bioconjugate.
Bioconjug Chem
; 23(3): 330-5, 2012 Mar 21.
Article
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| MEDLINE
| ID: mdl-22329542
ABSTRACT
Ethylene cross-bridged cyclam with two acetate pendant arms, ECB-TE2A, is known to form the most kinetically stable (64)Cu complexes. However, its usefulness as a bifunctional chelator is limited because of its harsh radiolabeling conditions. Herein, we report new cross-bridged cyclam chelator for the development of ultrastable (64)Cu-radiolabeled bioconjugates. Propylene cross-bridged TE2A (PCB-TE2A) was successfully synthesized in an efficient way. The Cu(II) complex of PCB-TE2A exhibited much higher kinetic stability than ECB-TE2A in acid decomplexation studies, and also showed high resistance to reduction-mediated demetalation. Furthermore, the quantitative radiolabeling of PCB-TE2A with (64)Cu was achieved under milder conditions compared to ECB-TE2A. Biodistribution studies strongly indicate that the (64)Cu complexes of PCB-TE2A cleared out rapidly from the body with minimum decomplexation.
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1
Banco de datos:
MEDLINE
Asunto principal:
Radioisótopos de Cobre
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Quelantes
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Compuestos Macrocíclicos
Límite:
Animals
Idioma:
En
Año:
2012
Tipo del documento:
Article