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Rapid Screening of Lectins for Multivalency Effects with a Glycodendrimer Microarray

  1. Núria Parera Pera Dr.1,
  2. Hilbert M. Branderhorst Dr.1,
  3. Raymond Kooij1,
  4. Caroline Maierhofer Dr.2,
  5. Marjolein van der Kaaden1,
  6. Rob M. J. Liskamp Prof. Dr.1,
  7. Valentin Wittmann Prof. Dr.2,
  8. Rob Ruijtenbeek Dr.3,
  9. Roland J. Pieters Dr.1

Article first published online: 29 JUL 2010

DOI: 10.1002/cbic.201000340

Issue

ChemBioChem

ChemBioChem

Volume 11, Issue 13, pages 1896–1904, September 3, 2010

Additional Information

How to Cite

Parera Pera, N., Branderhorst, H. M., Kooij, R., Maierhofer, C., van der Kaaden, M., Liskamp, R. M. J., Wittmann, V., Ruijtenbeek, R. and Pieters, R. J. (2010), Rapid Screening of Lectins for Multivalency Effects with a Glycodendrimer Microarray. ChemBioChem, 11: 1896–1904. doi: 10.1002/cbic.201000340

Author Information

  1. 1

    Department of Medicinal Chemistry and Chemical Biology, Utrecht Institute for Pharmaceutical Sciences, Utrecht University, P. O. Box 80082, 3508 TB Utrecht (The Netherlands), Fax: (+31) 30-2536944

  2. 2

    Universität Konstanz, Fachbereich Chemie, Fach 709, 78457 Konstanz (Germany)

  3. 3

    Pamgene International B.V. P. O. Box 1335, 5200 BJ 's-Hertogenbosch (The Netherlands)

Publication History

  1. Issue published online: 30 AUG 2010
  2. Article first published online: 29 JUL 2010
  3. Manuscript Received: 11 JUN 2010

Funded by

  • Dutch Technology Foundation STW
  • Ministry of Economic Affairs
  • Deutsche Forschungsgemeinschaft. Grant Number: FOR 434
  • Konstanz Research School Chemical Biology

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Keywords:

  • carbohydrates;
  • click chemistry;
  • dendrimers;
  • inhibitors;
  • microarrays

Graphical Abstract

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Nothing like the sum: A method for rapidly screening glycodendrimers on a chip was used to quickly identify potent multivalent inhibitors that might be important drug leads or might become part of sensitive sensing systems. Very distinct binding patterns were seen for the various lectins.

Abstract

Multivalency is an important phenomenon in protein–carbohydrate interactions. In order to evaluate glycodendrimers as multivalent inhibitors of carbohydrate binding proteins, we displayed them on a microarray surface. Valencies were varied from 1 to 8, and corrections were made for the valencies so that all surfaces contained the same amount of the sugar ligand. Five different carbohydrates were attached to the dendrimers. A series of fluorescent lectins was evaluated, and for each of them a binding profile was obtained from a single experiment showing both the specificity of the lectin for a certain sugar and whether it prefers multivalent ligands or not. Very distinct binding patterns were seen for the various lectins. The results were rationalized with respect to the interbinding distances of the lectins.

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