期刊
CHEMBIOCHEM
卷 18, 期 24, 页码 2428-2440出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cbic.201700544
关键词
binding studies; fluorescence polarization; galectin; inhibitors; lactosamine; microarrays
资金
- Fondation pour la Recherche Medicale [DCM20121225750]
- Japan Society for the Promotion of Science (JSPS)
- European Commission
- Education, Audiovisual and Culture Executive Agency (EACEA)
- Erasmus Mundus Joint Doctorate in nanomedicine and innovation in pharmaceutical sciences (NanoFar)
- Region Pays de la Loire (ReMSIP project)
- Laboratoires Servier
- Grants-in-Aid for Scientific Research [16H05071] Funding Source: KAKEN
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 typeII 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 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.
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