title: Supramolecular glycodendrimer-based hybrid drugs.
abstract: Specific noncovalent interactions are commonly used by nature to modulate numerous processes including cell recognition, viral adhesion, and transmembrane communications. Here we report on the design, synthesis, and preliminary characterization of new supramolecular glycodendrimer-based hybrid drugs based on adamantyl-modified glycodendrimers of third, fourth, or fifth generation (mPPI-G3-AdaB, mPPI-G4-AdaB, and mPPI-G5-AdaB) and a new heterobifunctional ligand. This component was tailored to bind through noncovalent interactions both the multimeric natural 5-HT3 receptor (through an optimized arylpiperazine pharmacophore) and the adamantyl groups located on the glycodendrimer surfaces (through a β-cyclodextrin residue) giving rise to biorelevant supramolecular constructs.
authors.affiliation: Dipartimento di Biotecnologie, Chimica e Farmacia and European Research Centre for Drug Discovery and Development, Università degli Studi di Siena , Via A. Moro 2, 53100 Siena, Italy.
authors.forename: Marco
authors.initials: M
authors.lastname: Paolino
authors.forename: Hartmut
authors.initials: H
authors.lastname: Komber
authors.forename: Laura
authors.initials: L
authors.lastname: Mennuni
authors.forename: Gianfranco
authors.initials: G
authors.lastname: Caselli
authors.forename: Dietmar
authors.initials: D
authors.lastname: Appelhans
authors.forename: Brigitte
authors.initials: B
authors.lastname: Voit
authors.forename: Andrea
authors.initials: A
authors.lastname: Cappelli
mesh_terms: D000818:Animals; D050091:Dendrimers / Q000737:chemistry* / Q000378:metabolism*; D046911:Macromolecular Substances / Q000737:chemistry / Q000378:metabolism; D008297:Male; D011485:Protein Binding / Q000502:physiology; D051381:Rats; D017208:Rats, Wistar; D044406:Receptors, Serotonin, 5-HT3 / Q000378:metabolism; D047392:beta-Cyclodextrins / Q000737:chemistry* / Q000378:metabolism*
chemical_list: D050091:Dendrimers; D046911:Macromolecular Substances; D044406:Receptors, Serotonin, 5-HT3; D047392:beta-Cyclodextrins