1h3c
From Proteopedia
(New page: 200px<br /> <applet load="1h3c" size="450" color="white" frame="true" align="right" spinBox="true" caption="1h3c, resolution 2.9Å" /> '''STRUCTURES OF HUMAN ...) |
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==About this Structure== | ==About this Structure== | ||
| - | 1H3C is a [[http://en.wikipedia.org/wiki/Single_protein Single protein]] structure of sequence from [[http://en.wikipedia.org/wiki/Alicyclobacillus_acidocaldarius Alicyclobacillus acidocaldarius]] with C8E and R79 as [[http://en.wikipedia.org/wiki/ligands ligands]]. Full crystallographic information is available from [[http://ispc.weizmann.ac.il/oca-bin/ocashort?id=1H3C OCA]]. | + | 1H3C is a [[http://en.wikipedia.org/wiki/Single_protein Single protein]] structure of sequence from [[http://en.wikipedia.org/wiki/Alicyclobacillus_acidocaldarius Alicyclobacillus acidocaldarius]] with C8E and R79 as [[http://en.wikipedia.org/wiki/ligands ligands]]. Structure known Active Site: AC1. Full crystallographic information is available from [[http://ispc.weizmann.ac.il/oca-bin/ocashort?id=1H3C OCA]]. |
==Reference== | ==Reference== | ||
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[[Category: oxidosqualene cyclase]] | [[Category: oxidosqualene cyclase]] | ||
| - | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Tue Oct 30 12:30:10 2007'' |
Revision as of 10:25, 30 October 2007
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STRUCTURES OF HUMAN OXIDOSQUALENE CYCLASE INHIBITORS BOUND TO A HOMOLGOUS ENZYME
Overview
The binding structures of 11 human oxidosqualene cyclase inhibitors, designed as cholesterol-lowering agents were determined for the, squalene-hopene cyclase from Alicyclobacillus acidocaldarius, which is the, only structurally known homologue of the human enzyme. The complexes were, produced by cocrystallization, and the structures were elucidated by X-ray, diffraction analyses. All inhibitors were bound in the large active center, cavity. The detailed binding structures are presented and discussed in the, light of the IC50 values of these 11 as well as 17 other inhibitors. They, provide a consistent picture for the inhibition of the bacterial enzyme, and can be used to adjust and improve homology models of the human enzyme., The detailed active center structures of the two enzymes are ... [(full description)]
About this Structure
1H3C is a [Single protein] structure of sequence from [Alicyclobacillus acidocaldarius] with C8E and R79 as [ligands]. Structure known Active Site: AC1. Full crystallographic information is available from [OCA].
Reference
Binding structures and potencies of oxidosqualene cyclase inhibitors with the homologous squalene-hopene cyclase., Lenhart A, Reinert DJ, Aebi JD, Dehmlow H, Morand OH, Schulz GE, J Med Chem. 2003 May 22;46(11):2083-92. PMID:12747780
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