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Development of a Sensitive Microarray Platform for the Ranking of Galectin Inhibitors: Identification of a Selective Galectin‐3 Inhibitor
Author(s) -
Dion Johann,
Advedissian Tamara,
Storozhylova Nataliya,
Dahbi Samir,
Lambert Annie,
Deshayes Frédérique,
Viguier Mireille,
Tellier Charles,
Poirier Françoise,
Téletchéa Stéphane,
Dussouy Christophe,
Tateno Hiroaki,
Hirabayashi Jun,
Grandjean Cyrille
Publication year - 2017
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.201700544
Subject(s) - galectin , glycan , chemistry , oxazoline , lectin , glycosylation , microarray , galectin 3 , glycoproteomics , biochemistry , computational biology , combinatorial chemistry , glycoprotein , biology , gene , gene expression , immunology , catalysis
Glycan microarrays are useful tools for lectin glycan profiling. The use of a glycan microarray based on evanescent‐field fluorescence detection was herein further extended to the screening of lectin inhibitors in competitive experiments. The efficacy of this approach was tested with 2/3′‐mono‐ and 2,3′‐diaromatic type II lactosamine derivatives and galectins as targets and was validated by comparison with fluorescence anisotropy proposed as an orthogonal protein interaction measurement technique. We showed that subtle differences in the architecture of the inhibitor could be sensed that pointed out the preference of galectin‐3 for 2′‐arylamido derivatives over ureas, thioureas, and amines and that of galectin‐7 for derivatives bearing an α substituent at the anomeric position of glucosamine. We eventually identified a diaromatic oxazoline as a highly specific inhibitor of galectin‐3 versus galectin‐1 and galectin‐7.