Multifunctional multivalency: a focused library of polymeric cholera toxin antagonists
- ️David R. Bundle
* Corresponding authors
a
Alberta Ingenuity Centre for Carbohydrate Science, Department of Chemistry, University of Alberta, Edmonton, Alberta, Canada
E-mail:
dave.bundle@ualberta.ca
Fax: (+1)780-492-7705
Tel: (+1)780-492-8808
b TheraCarb Inc., 243-3553 31st Street N.W., Calgary, Alberta, Canada
Abstract
Structural pre-organization of the multivalent ligands is important for successful interaction with multimeric proteins. Polymer-based heterobifunctional ligands that contain pendant groups prearranged into heterodimers can be used to probe the active site and surrounding area of the receptor. Here we describe the synthesis and activities of a series of galactose conjugates on polyacrylamide and dextran. Conjugation of a second fragment resulted in nanomolar inhibitors of cholera toxin, while the galactose-only progenitors showed no detectable activity.
Supplementary files
Article information
- https://doi.org/10.1039/C0OB01089H
- Paper
- 26 Nov 2010
- 09 Feb 2011
- 10 Feb 2011
DOI
Article type
Submitted
Accepted
First published
Org. Biomol. Chem., 2011,9, 3658-3671
Permissions
Multifunctional multivalency: a focused library of polymeric cholera toxin antagonists
H. Tran, P. I. Kitov, E. Paszkiewicz, J. M. Sadowska and D. R. Bundle, Org. Biomol. Chem., 2011, 9, 3658 DOI: 10.1039/C0OB01089H
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