Selectin Antagonists May Help Treat Inflammation

(University of Basel, July 10, 2013)

Uni Basel researchers have identified a new class of selectin antagonists as lead structures for anti-inflammatory drugs, as published in the Journal of the American Chemical Society. The selectins (C-type lectins) are biologically important, since they present attractive therapeutic targets in diseases involving cell adhesion, extravasation of cells from the bloodstream, or the migration of specific lymphocytes. Sialyl Lewisx (sLex) is the carbohydrate epitope recognized by E-selectin. The sLex/E-selectin interaction has low affinity and a short half-life, which makes it difficult to develop selectin antagonists for therapeutic applications. Using nuclear magnetic resonance, the researchers identified fragments binding to a second site near the sLex binding site. With GlycoMimetics Inc., the team has successfully promoted a selectin antagonist to clinical trials.