Oligopresentation of protease inhibitors with β-cyclodextrin as template

Perfacial functionalization of β-cyclodextrin as heptakis-(6-mercapto-6-deoxy)- and heptakis-(6-succinylamido-6-deoxy)-derivative was used to graft the tripeptide aldehyde Leu-Leu-Nle-H to the strongly solubilizing carbohydrate template. Oligopresentation of this inhibitor and thus in loco increase of the concentration was not found to enhance inhibition of cathepsin B and μ-calpain on molar basis if compared to the mono-conjugated form.