Multifunctional multivalency: a focused library of polymeric cholera toxin antagonists |
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Authors: | Tran Huu-Anh Kitov Pavel I Paszkiewicz Eugenia Sadowska Joanna M Bundle David R |
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Institution: | Alberta Ingenuity Centre for Carbohydrate Science, Department of Chemistry, University of Alberta, Edmonton, Alberta, Canada. |
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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. |
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