1gsz

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[[Image:1gsz.gif|left|200px]]
[[Image:1gsz.gif|left|200px]]
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{{Structure
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|PDB= 1gsz |SIZE=350|CAPTION= <scene name='initialview01'>1gsz</scene>, resolution 2.8&Aring;
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The line below this paragraph, containing "STRUCTURE_1gsz", creates the "Structure Box" on the page.
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|SITE= <scene name='pdbsite=C8A:R71+Binding+Site+For+Chain+C'>C8A</scene>
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=C8E:(HYDROXYETHYLOXY)TRI(ETHYLOXY)OCTANE'>C8E</scene>, <scene name='pdbligand=R71:[4-({6-[ALLYL(METHYL)AMINO]HEXYL}OXY)-2-FLUOROPHENYL](4-BROMOPHENYL)METHANONE'>R71</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|GENE=
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{{STRUCTURE_1gsz| PDB=1gsz | SCENE= }}
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|RELATEDENTRY=
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1gsz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1gsz OCA], [http://www.ebi.ac.uk/pdbsum/1gsz PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1gsz RCSB]</span>
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}}
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'''CRYSTAL STRUCTURE OF A SQUALENE CYCLASE IN COMPLEX WITH THE POTENTIAL ANTICHOLESTEREMIC DRUG RO48-8071'''
'''CRYSTAL STRUCTURE OF A SQUALENE CYCLASE IN COMPLEX WITH THE POTENTIAL ANTICHOLESTEREMIC DRUG RO48-8071'''
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[[Category: Schulz, G E.]]
[[Category: Schulz, G E.]]
[[Category: Weihofen, W A.]]
[[Category: Weihofen, W A.]]
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[[Category: cholesterol biosynthesis]]
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[[Category: Cholesterol biosynthesis]]
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[[Category: inhibitor interaction]]
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[[Category: Inhibitor interaction]]
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[[Category: isomerase]]
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[[Category: Isomerase]]
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[[Category: monotopic membrane protein]]
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[[Category: Monotopic membrane protein]]
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[[Category: oxidosqualene cyclase]]
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[[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 Sun Mar 30 20:50:36 2008''
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Revision as of 14:58, 2 May 2008

Image:1gsz.gif

Template:STRUCTURE 1gsz

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


Overview

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.

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 Fri May 2 17:58:07 2008

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