This week in therapeutics




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Cancer; inflammation

E selectin (SELE; CD62E)

In vitro studies suggest nitroindole-triazole analogs of a tetrasaccharide sialyl Lewisx (sLex) mimic could help treat cancer and inflammatory diseases. sLex is the minimum carbohydrate epitope required for inhibitory binding to SELE, which has been linked to cancer and inflammatory diseases. A series of in vitro assays identified nitroindole-triazole analogs of an sLex mimic that bound SELE with low nanomolar affinities. In these assays, the lead analogs also showed >200-fold longer SELE binding half-lives compared with the unmodified mimic. Next steps could include testing the compounds in animal models for cancer and inflammatory disease.
GlycoMimetics Inc. and Pfizer Inc. have
GMI-1070, a glycomimetic inhibitor of SELE, SELP (CD62P) and SELL (CD62L), in Phase II trials to treat sickle cell disease.
GlycoMimetics' SELE inhibitor GMI-1271 is in preclinical testing to treat acute myelogenous leukemia (AML) and thrombosis.

SciBX 6(27); doi:10.1038/scibx.2013.695
Published online July 18, 2013

Patented by the University of Basel; licensed to GlycoMimetics

Egger, J. et al. J. Am. Chem. Soc.; published online June 6, 2013;
Contact: Beat Ernst, University of Basel, Basel, Switzerland