Derivatizations of Sgc8-c aptamer to prepare metallic radiopharmaceuticals as imaging diagnostic agents: Syntheses, isolations and physicochemical characterizations

Abstract

Aptamers, oligonucleotides with the capability to bind to a target through non-covalent bonds with high affinity and specificity, have a great number of advantages as scaffold to prepare molecular imaging agents. In this sense, we have performed post-SELEX modifications of a truncated aptamer, Sgc8-c, which bind to protein tyrosine kinase 7 to obtain a specific molecular targeting probe for in vivo-diagnosis and -therapy. Herein, we describe the synthetic efforts to prepare conjugates between Sgc8-c and different metallic ions chelator-moieties in short times, high purities, and adequate yields. The selected chelator-moieties, derived from 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA), 2-benzyl-1,4,7-triazacyclononane-1,4,7-triacetic acid (NOTA) and 6-hydrazinonicotinic acid (HYNIC), were covalently attached at the 5′-aptamer position yielding the expected products which were stables in aqueous solution up to 75 °C and in typical aptamers-storages conditions at least for 30 days.

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Post-SELEX modification on Sgc8-c aptamer, in order to prepare conjugate for furthrer transformations to radiopharmaceuticals, are described

Derivatizations of Sgc8-c aptamer to prepare metallic radiopharmaceuticals as imaging diagnostic agents: Syntheses, isolations and physicochemical characterizations

Estefanía Sicco, Jessica Báez, Jimena Margenat, Fernanda García, Manuel ibarra, Pablo Cabral, María Moreno, Hugo Cerecetto* and Victoria Calzada*

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