Fine tuning of beta-glucosidase inhibitory activity in the 2,5-dideoxy-2,5-imino-D-mannitol (DMDP) system.
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.
Wrodnigg
Tanja M
TM
Glycogroup, Institut für Organische Chemie der Technischen Universität Graz, Stremayrgasse 16, A-8010 Graz, Austria. t.wrodnigg@tu-graz.ac.at
Stütz
Arnold E
AE
Tarling
Chris A
CA
Withers
Stephen G
SG
D050112:Imino Pyranoses / Q000494:pharmacology; D007700:Kinetics; D008353:Mannitol / Q000031:analogs & derivatives* / Q000494:pharmacology; D012231:Rhizobium / Q000201:enzymology; D013329:Structure-Activity Relationship; D001617:beta-Glucosidase / Q000037:antagonists & inhibitors*
C494911:2,5-dideoxy-2,5-imino-D-mannitol; D050112:Imino Pyranoses; D008353:Mannitol; D001617:beta-Glucosidase