Strong inhibition of cholera toxin by multivalent GM1 derivatives

Aliaksei V. Pukin; Hilbert M. Branderhorst; Cristina Sisu; Carel A. G. M. Weijers; Michel Gilbert; Rob M. J. Liskamp; Gerben M. Visser; Han Zuilhof; Roland J. Pieters

doi:10.1002/cbic.200700266

Strong inhibition of cholera toxin by multivalent GM1 derivatives

Aliaksei V. Pukin, Hilbert M. Branderhorst, Cristina Sisu, Carel A. G. M. Weijers, Michel Gilbert, Rob M. J. Liskamp, Gerben M. Visser, Han Zuilhof, Roland J. Pieters

Dept of Pharmaceutical Sciences

Research output: Contribution to journal › Article › Academic › peer-review

Abstract

(Chemical Equation Presented) 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. © 2007 Wiley-VCH Verlag GmbH & Co. KGaA.

Original language	English
Pages (from-to)	1500-1503
Number of pages	4
Journal	ChemBioChem
Volume	8
Issue number	13
DOIs	https://doi.org/10.1002/cbic.200700266
Publication status	Published - 3 Sept 2007

Keywords

Dendrimers
Glycoconjugates
Ligand design
Oligosaccharides
alpha galactopyranoside
cholera toxin B subunit
enterotoxin
ganglioside GM1
pyranoside
unclassified drug
article
binding affinity
drug activity
drug inhibition
human
priority journal
protein binding

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1002/cbic.200700266

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title = "Strong inhibition of cholera toxin by multivalent GM1 derivatives",

abstract = "(Chemical Equation Presented) 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. {\textcopyright} 2007 Wiley-VCH Verlag GmbH & Co. KGaA.",

keywords = "Dendrimers, Glycoconjugates, Ligand design, Oligosaccharides, alpha galactopyranoside, cholera toxin B subunit, enterotoxin, ganglioside GM1, pyranoside, unclassified drug, article, binding affinity, drug activity, drug inhibition, human, priority journal, protein binding",

author = "Pukin, {Aliaksei V.} and Branderhorst, {Hilbert M.} and Cristina Sisu and Weijers, {Carel A. G. M.} and Michel Gilbert and Liskamp, {Rob M. J.} and Visser, {Gerben M.} and Han Zuilhof and Pieters, {Roland J.}",

year = "2007",

month = sep,

day = "3",

doi = "10.1002/cbic.200700266",

language = "English",

volume = "8",

pages = "1500--1503",

journal = "ChemBioChem",

issn = "1439-4227",

publisher = "John Wiley and Sons Inc.",

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TY - JOUR

T1 - Strong inhibition of cholera toxin by multivalent GM1 derivatives

AU - Pukin, Aliaksei V.

AU - Branderhorst, Hilbert M.

AU - Sisu, Cristina

AU - Weijers, Carel A. G. M.

AU - Gilbert, Michel

AU - Liskamp, Rob M. J.

AU - Visser, Gerben M.

AU - Zuilhof, Han

AU - Pieters, Roland J.

PY - 2007/9/3

Y1 - 2007/9/3

N2 - (Chemical Equation Presented) 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. © 2007 Wiley-VCH Verlag GmbH & Co. KGaA.

AB - (Chemical Equation Presented) 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. © 2007 Wiley-VCH Verlag GmbH & Co. KGaA.

KW - Dendrimers

KW - Glycoconjugates

KW - Ligand design

KW - Oligosaccharides

KW - alpha galactopyranoside

KW - cholera toxin B subunit

KW - enterotoxin

KW - ganglioside GM1

KW - pyranoside

KW - unclassified drug

KW - article

KW - binding affinity

KW - drug activity

KW - drug inhibition

KW - human

KW - priority journal

KW - protein binding

U2 - 10.1002/cbic.200700266

DO - 10.1002/cbic.200700266

M3 - Article

SN - 1439-4227

VL - 8

SP - 1500

EP - 1503

JO - ChemBioChem

JF - ChemBioChem

IS - 13

ER -

Strong inhibition of cholera toxin by multivalent GM1 derivatives

Abstract

Keywords

UN SDGs

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