2. Academic Validation
  3. Design and synthesis of a new sialyl Lewis X mimetic: how selective are the selectin receptors?

Design and synthesis of a new sialyl Lewis X mimetic: how selective are the selectin receptors?

  • Bioorg Med Chem Lett. 2001 May 7;11(9):1109-12. doi: 10.1016/s0960-894x(01)00130-5.
M De Vleeschauwer 1,  M Vaillancourt,  N Goudreau,  Y Guindon,  D Gravel
Affiliations

Affiliation

  • 1 Départment de chimie, Université de Montréal, Québec, Canada.
PMID: 11354355 DOI: 10.1016/s0960-894x(01)00130-5
Abstract

The present paper reports the molecular modeling-based design and synthesis of an optically pure noncarbohydrate mimetic of sialyl Lewis X to inhibit E-Selectin. Biological evaluation of the designed substance as well as that of its enantiomer gave, contrary to expectations, comparable IC50 values. Results are discussed in terms of receptor binding specificity and the molecular modeling protocol used.

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