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Derivatizations of Sgc8‐c aptamer to prepare metallic radiopharmaceuticals as imaging diagnostic agents: Syntheses, isolations, and physicochemical characterizations
Author(s) -
Sicco Estefanía,
Báez Jessica,
Margenat Jimena,
García Fernanda,
Ibarra Manuel,
Cabral Pablo,
Moreno María,
Cerecetto Hugo,
Calzada Victoria
Publication year - 2018
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.13135
Subject(s) - aptamer , chemistry , combinatorial chemistry , nanotechnology , microbiology and biotechnology , materials science , biology
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 in vivo 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, 2‐benzyl‐1,4,7‐triazacyclononane‐1,4,7‐triacetic acid, and 6‐hydrazinonicotinic acid, were covalently attached at the 5′‐aptamer position yielding the expected products which were stable in aqueous solution up to 75°C and in typical aptamer storage conditions at least for 30 days.