1h3c

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{{Seed}}
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{{STRUCTURE_1h3c| PDB=1h3c | SCENE= }}
{{STRUCTURE_1h3c| PDB=1h3c | SCENE= }}
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'''STRUCTURES OF HUMAN OXIDOSQUALENE CYCLASE INHIBITORS BOUND TO A HOMOLGOUS ENZYME'''
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===STRUCTURES OF HUMAN OXIDOSQUALENE CYCLASE INHIBITORS BOUND TO A HOMOLGOUS ENZYME===
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==Overview==
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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 too different to show an IC50 correlation.
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(as it appears on PubMed at http://www.pubmed.gov), where 12747780 is the PubMed ID number.
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{{ABSTRACT_PUBMED_12747780}}
==About this Structure==
==About this Structure==
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[[Category: Monotopic membrane]]
[[Category: Monotopic membrane]]
[[Category: Oxidosqualene cyclase]]
[[Category: Oxidosqualene cyclase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 18:22:50 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 1 06:33:28 2008''

Revision as of 03:33, 1 July 2008

Image:1h3c.png

Template:STRUCTURE 1h3c

STRUCTURES OF HUMAN OXIDOSQUALENE CYCLASE INHIBITORS BOUND TO A HOMOLGOUS ENZYME

Template:ABSTRACT PUBMED 12747780

About this Structure

1H3C is a Single protein structure of sequence from Alicyclobacillus acidocaldarius. 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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