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1gsz

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{{STRUCTURE_1gsz| PDB=1gsz | SCENE= }}
{{STRUCTURE_1gsz| PDB=1gsz | SCENE= }}
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'''CRYSTAL STRUCTURE OF A SQUALENE CYCLASE IN COMPLEX WITH THE POTENTIAL ANTICHOLESTEREMIC DRUG RO48-8071'''
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===CRYSTAL STRUCTURE OF A SQUALENE CYCLASE IN COMPLEX WITH THE POTENTIAL ANTICHOLESTEREMIC DRUG RO48-8071===
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==Overview==
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Squalene-hopene cyclase (SHC) catalyzes the conversion of squalene into pentacyclic compounds. It is the prokaryotic counterpart of the eukaryotic oxidosqualene cyclase (OSC) that catalyzes the steroid scaffold formation. Because of clear sequence homology, SHC can serve as a model for OSC, which is an attractive target for anticholesteremic drugs. We have established the crystal structure of SHC complexed with Ro48-8071, a potent inhibitor of OSC and therefore of cholesterol biosynthesis. Ro48-8071 is bound in the active-center cavity of SHC and extends into the channel that connects the cavity with the membrane. The binding site of Ro48-8071 is largely identical with the expected site of squalene; it differs from a previous model based on photoaffinity labeling. The knowledge of the inhibitor binding mode in SHC is likely to help develop more potent inhibitors for OSC.
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(as it appears on PubMed at http://www.pubmed.gov), where 12031670 is the PubMed ID number.
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{{ABSTRACT_PUBMED_12031670}}
==About this Structure==
==About this Structure==
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[[Category: Monotopic membrane protein]]
[[Category: Monotopic membrane protein]]
[[Category: Oxidosqualene cyclase]]
[[Category: Oxidosqualene cyclase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 17:58:07 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 1 06:01:32 2008''

Revision as of 03:01, 1 July 2008

Image:1gsz.png

Template:STRUCTURE 1gsz

CRYSTAL STRUCTURE OF A SQUALENE CYCLASE IN COMPLEX WITH THE POTENTIAL ANTICHOLESTEREMIC DRUG RO48-8071

Template:ABSTRACT PUBMED 12031670

About this Structure

1GSZ is a Single protein structure of sequence from Alicyclobacillus acidocaldarius. Full crystallographic information is available from OCA.

Reference

Crystal structure of a squalene cyclase in complex with the potential anticholesteremic drug Ro48-8071., Lenhart A, Weihofen WA, Pleschke AE, Schulz GE, Chem Biol. 2002 May;9(5):639-45. PMID:12031670

Page seeded by OCA on Tue Jul 1 06:01:32 2008

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