Medizinische Universität Graz Austria/Österreich - Forschungsportal - Medical University of Graz
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SHR Neuro Krebs Kardio Lipid Stoffw Microb
Wolfsgruber, A; Thonhofer, M; Weber, P; Nasseri, SA; Fischer, R; Schalli, M; Stütz, AE; Withers, SG; Wrodnigg, TM.
N-Alkylated Iminosugar Based Ligands: Synthesis and Inhibition of Human Lysosomal β-Glucocerebrosidase.
Molecules. 2020; 25(20):
Doi: 10.3390/molecules25204618
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- Schalli Michael
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- Abstract:
- The scope of a series of N-alkylated iminosugar based inhibitors in the d-gluco as well as d-xylo configuration towards their interaction with human lysosomal β-glucocerebrosidase has been evaluated. A versatile synthetic toolbox has been developed for the synthesis of N-alkylated iminosugar scaffolds conjugated to a variety of terminal groups via a benzoic acid ester linker. The terminal groups such as nitrile, azide, alkyne, nonafluoro-tert-butyl and amino substituents enable follow-up chemistry as well as visualisation experiments. All compounds showed promising inhibitory properties as well as selectivities for β-glucosidases, some exhibiting activities in the low nanomolar range for β-glucocerebrosidase.
- Find related publications in this database (Keywords)
- N-alkylated iminosugars
- inhibitors for β
- -glucocerebrosidase
- tools for glycoprocessing enzymes
- β
- -glucosidase inhibitors
- glycomimetics