Multivalent supramolecular dendrimer-based drugs.
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.
Galeazzi
Simone
S
Dipartimento Farmaco Chimico Tecnologico and European Research Centre for Drug Discovery and Development, Universitàà di Siena, Via A. Moro, 53100 Siena, Italy.
Hermans
Thomas M
TM
Paolino
Marco
M
Anzini
Maurizio
M
Mennuni
Laura
L
Giordani
Antonio
A
Caselli
Gianfranco
G
Makovec
Francesco
F
Meijer
E W
EW
Vomero
Salvatore
S
Cappelli
Andrea
A
D050091:Dendrimers / Q000737:chemistry* / Q000378:metabolism*; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D044406:Receptors, Serotonin, 5-HT3 / Q000378:metabolism*; D014867:Water / Q000737:chemistry* / Q000378:metabolism
D050091:Dendrimers; D044406:Receptors, Serotonin, 5-HT3; D014867:Water