Dendrimer-based dynamic combinatorial libraries

ORGN 30

Theresa Chang, t.c.chang@tue.nl and E. W. Meijer. Laboratory of Macromolecular and Organic Chemistry, Eindhoven University of Technology, P.O. Box 513, 5600 MB, 5600 MB Eindhoven, Netherlands
The aim of this project is to create water-soluble dynamic combinatorial libraries based upon dendrimer-guest complexes. The guest molecules are designed to bind to dendrimers using multiple secondary interactions, such as electrostatics and hydrogen bonding. We have been able to incorporate various guest molecules into the fifth generation adamantyl-urea terminated dendrimer (DAB), including peptides, provided that they are appended with an acid-urea group. These guest molecules also serve to solubilize the otherwise insoluble dendrimer in water. These dendrimer-guest complexes have been shown to be stable in water. The guest molecules displayed at the periphery of the dendrimer can then bind to a receptor (protein) in a multivalent fashion. The aggregation behavior of the dendrimer-guest complexes and receptors can be studied using AFM and fluorescence measurements.