1oim
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FAMILY 1 B-GLUCOSIDASE FROM THERMOTOGA MARITIMA
OverviewOverview
The design and synthesis of transition-state mimics reflects the growing, need both to understand enzymatic catalysis and to influence strategies, for therapeutic intervention. Iminosugars are among the most potent, inhibitors of glycosidases. Here, the binding of 1-deoxynojirimycin and, (+)-isofagomine to the "family GH-1" beta-glucosidase of Thermotoga, maritima is investigated by kinetic analysis, isothermal titration, calorimetry, and X-ray crystallography. The binding of both of these, iminosugar inhibitors is driven by a large and favorable enthalpy. The, greater inhibitory power of isofagomine, relative to 1-deoxynojirimycin, however, resides in its significantly more favorable entropy; indeed the, differing thermodynamic signatures of these inhibitors are further, highlighted by ... [(full description)]
About this StructureAbout this Structure
1OIM is a [Single protein] structure of sequence from [Thermotoga maritima] with NOJ as [ligand]. Active as [Beta-glucosidase], with EC number [3.2.1.21]. Structure known Active Site: AC1. Full crystallographic information is available from [OCA].
ReferenceReference
Iminosugar glycosidase inhibitors: structural and thermodynamic dissection of the binding of isofagomine and 1-deoxynojirimycin to beta-glucosidases., Zechel DL, Boraston AB, Gloster T, Boraston CM, Macdonald JM, Tilbrook DM, Stick RV, Davies GJ, J Am Chem Soc. 2003 Nov 26;125(47):14313-23. PMID:14624580
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