Medizinische Universität Graz Austria/Österreich - Forschungsportal - Medical University of Graz
Gewählte Publikation:
SHR Neuro Krebs Kardio Lipid Stoffw Microb
Schitter, G; Steiner, AJ; Pototschnig, G; Scheucher, E; Thonhofer, M; Tarling, CA; Withers, SG; Fantur, K; Paschke, E; Mahuran, DJ; Rigat, BA; Tropak, MB; Illaszewicz, C; Saf, R; Stutz, AE; Wrodnigg, TM.
Fluorous iminoalditols: a new family of glycosidase inhibitors and pharmacological chaperones.
Chembiochem. 2010; 11(14):2026-2033
Doi: 10.1002/cbic.201000192
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- Co-Autor*innen der Med Uni Graz
- Fantur Katrin Medea-Emma
- Paschke Eduard
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- Abstract:
- A collection of new reversible glycosidase inhibitors of the iminoalditol type featuring N-substituents containing perfluorinated regions has been prepared for evaluation of physicochemical, biochemical and diagnostic properties. The vast variety of feasible oligofluoro moieties allows for modular approaches to customised structures according to the intended applications, which are influenced by the fluorine content as well as the distance of the fluorous moiety from the ring nitrogen. The first examples, in particular in the D-galacto series, exhibited excellent inhibitory activities. A preliminary screen with two human cell lines showed that, at subinhibitory concentrations, they are powerful pharmacological chaperones enhancing the activities of the catalytically handicapped lysosomal D-galactosidase mutants associated with GM1 gangliosidosis and Morquio B disease.
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- Find related publications in this database (Keywords)
- chaperones
- enzymes
- fluorine
- glycosidases
- inhibitors