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Multivalent supramolecular dendrimer-based drugs. 2010
Simone Galeazzi, and
Thomas M Hermans, and
Marco Paolino, and
Maurizio Anzini, and
Laura Mennuni, and
Antonio Giordani, and
Gianfranco Caselli, and
Francesco Makovec, and
E W Meijer, and
Salvatore Vomero, and
Andrea Cappelli
Dipartimento Farmaco Chimico Tecnologico and European Research Centre for Drug Discovery and Development, Universitàà di Siena, Via A. Moro, 53100 Siena, Italy.
Supramolecular complexes consisting of a hydrophobic dendrimer host [DAB-dendr-(NHCONH-Ad)(64)] as well as solubilizing and bioactive guest molecules have been synthesized using a noncovalent approach. The guest-host supramolecular assembly is first preassembled in chloroform and transferred via the neat phase to aqueous solution. The bioactive guest molecules can bind to a natural (serotonin 5-HT(3)) receptor with nanomolar affinity as well as to the synthetic dendrimer receptor in aqueous solution, going toward a dynamic multivalent supramolecular construct capable of adapting itself to a multimeric receptor motif.
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