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Strong Inhibition of Cholera Toxin by Multivalent GM1 Derivatives
Author(s) -
Pukin Aliaksei V.,
Branderhorst Hilbert M.,
Sisu Cristina,
Weijers Carel A. G. M.,
Gilbert Michel,
Liskamp Rob M. J.,
Visser Gerben M.,
Zuilhof Han,
Pieters Roland J.
Publication year - 2007
Publication title -
chembiochem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.05
H-Index - 126
eISSN - 1439-7633
pISSN - 1439-4227
DOI - 10.1002/cbic.200700266
Subject(s) - cholera toxin , toxin , chemistry , ligand (biochemistry) , derivative (finance) , stereochemistry , combinatorial chemistry , oligosaccharide , vibrio cholerae , biophysics , biochemistry , microbiology and biotechnology , biology , receptor , bacteria , genetics , financial economics , economics
Sticky fingers . The optimal ligand for the cholera toxin (CT), GM1‐oligosaccharide (GM1os), was linked to dendritic structures that contained long spacer arms by using highly efficient “click” chemistry coupling. In the inhibition studies very large multivalency effects were observed; the best structure was an unprecedented 380 000‐fold more potent ligand for the toxin than a monovalent GM1os derivative.