2ceq
From Proteopedia
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| - | [[Image:2ceq.gif|left|200px]]<br /> | + | [[Image:2ceq.gif|left|200px]]<br /><applet load="2ceq" size="450" color="white" frame="true" align="right" spinBox="true" |
| - | <applet load="2ceq" size="450" color="white" frame="true" align="right" spinBox="true" | + | |
caption="2ceq, resolution 2.14Å" /> | caption="2ceq, resolution 2.14Å" /> | ||
'''BETA-GLYCOSIDASE FROM SULFOLOBUS SOLFATARICUS IN COMPLEX WITH GLUCOIMIDAZOLE'''<br /> | '''BETA-GLYCOSIDASE FROM SULFOLOBUS SOLFATARICUS IN COMPLEX WITH GLUCOIMIDAZOLE'''<br /> | ||
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==About this Structure== | ==About this Structure== | ||
| - | 2CEQ is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Sulfolobus_solfataricus Sulfolobus solfataricus] with ACT and GIM as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Beta-galactosidase Beta-galactosidase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.2.1.23 3.2.1.23] | + | 2CEQ is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Sulfolobus_solfataricus Sulfolobus solfataricus] with ACT and GIM as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Beta-galactosidase Beta-galactosidase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.2.1.23 3.2.1.23] Known structural/functional Site: <scene name='pdbsite=AC1:Gim Binding Site For Chain A'>AC1</scene>. Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2CEQ OCA]. |
==Reference== | ==Reference== | ||
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[[Category: hydrolase]] | [[Category: hydrolase]] | ||
| - | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Tue Dec 18 19:19:28 2007'' |
Revision as of 17:09, 18 December 2007
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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 by the phenethyl-substituted imidazole compound.
About this Structure
2CEQ is a Single protein structure of sequence from Sulfolobus solfataricus with ACT and GIM as ligands. Active as Beta-galactosidase, with EC number 3.2.1.23 Known structural/functional Site: . 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
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