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2ceq
From Proteopedia
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BETA-GLYCOSIDASE FROM SULFOLOBUS SOLFATARICUS IN COMPLEX WITH GLUCOIMIDAZOLE
Overview
Inhibition of glycosidases has great potential in the quest for highly, potent and specific drugs to treat diseases such as diabetes, cancer, and, viral infections. One of the most effective ways of designing such, compounds is by mimicking the transition state. Here we describe the, structural, kinetic, and thermodynamic dissection of binding of two, glucoimidazole-derived compounds, which are among the most potent, glycosidase inhibitors reported to date, with two family 1, beta-glycosidases. Provocatively, while inclusion of the phenethyl moiety, improves binding by a factor of 20-80-fold, this does not appear to result, from better noncovalent interactions with the enzyme; instead, improved, affinity may be derived from significantly better entropic contributions, to binding displayed ... [(full description)]
About this Structure
2CEQ is a [Single protein] structure of sequence from [Sulfolobus solfataricus] with ACT and GIM as [ligands]. Active as [[1]], with EC number [3.2.1.23]. Full crystallographic information is available from [OCA].
Reference
Structural, kinetic, and thermodynamic analysis of glucoimidazole-derived glycosidase inhibitors., Gloster TM, Roberts S, Perugino G, Rossi M, Moracci M, Panday N, Terinek M, Vasella A, Davies GJ, Biochemistry. 2006 Oct 3;45(39):11879-84. PMID:17002288
Page seeded by OCA on Mon Oct 29 20:53:07 2007
