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Start Over Author "Ernst, Beat" Journal bioorganic & medicinal chemistry
12 results on '"Ernst, Beat"'

12. Probing the carbohydrate recognition domain of E-selectin: The importance of the acid orientation in sLex mimetics

Author

Titz, Alexander, Patton, John, Smiesko, Martin, Radic, Zorana, Schwardt, Oliver, Magnani, John L., and Ernst, Beat

Subjects
*CARBOHYDRATE drugs, *SELECTINS, *LEUCOCYTES, *LIGANDS (Biochemistry), *INFLAMMATORY bowel diseases, *CARBOXYLIC acids
Abstract

Abstract: The selectin–leukocyte interaction is the initial event in the early inflammatory cascade. This interplay proceeds via the terminal tetrasaccharide sialyl Lewisx (sLex), present on physiological selectin ligands and E- and P-selectins located on the endothelial surface. Blocking this process is regarded as a promising therapeutic approach for inflammatory diseases where excessive leukocyte efflux is responsible for tissue damage. Selectin antagonists are generally based on sLex as lead structure, containing the essential pharmacophores pre-oriented in the bioactive conformation. In this work, we describe a set of competitive sLex mimetics possessing the carboxylic acid pharmacophore equipped with additional hydrophobic substituents as neuraminic acid (Neu5Ac) replacements. This small library of antagonists derived from Huisgen-1,3-dipolar cycloadditions allows to further probe the carbohydrate recognition domain of E-selectin. [Copyright &y& Elsevier]

Published
2010
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