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Fine tuning of beta-glucosidase inhibitory activity in the 2,5-dideoxy-2,5-imino-D-mannitol (DMDP) system
Authors:Wrodnigg Tanja M  Stütz Arnold E  Tarling Chris A  Withers Stephen G
Affiliation:Glycogroup, Institut für Organische Chemie der Technischen Universit?t Graz, Stremayrgasse 16, A-8010 Graz, Austria. t.wrodnigg@tu-graz.ac.at
Abstract:Based on our extensive studies of D-glucosidase inhibiting 2,5-dideoxy-2,5-imino-D-mannitol derivatives, we have been trying to create a series of fluorescent derivatives with a view to an 'inhibitory activity ruler' based on competitive displacement reactions of non-fluorescent inhibitors by fluorescent ones and vice versa, which can be performed and followed in microtiter plates or on-chips. Thus, a set of compounds was assembled with Ki values between 2 nM and 1 microM against Agrobacterium sp. beta-glucosidase.
Keywords:Glucosidase inhibitor   2,5-Dideoxy-2,5-imino-  smallcaps"  >d-mannitol   Fluorescent tag   Synthesis
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