1gsz
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(New page: 200px<br /> <applet load="1gsz" size="450" color="white" frame="true" align="right" spinBox="true" caption="1gsz, resolution 2.8Å" /> '''CRYSTAL STRUCTURE OF...)
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Revision as of 17:46, 29 October 2007
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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 ... [(full description)]
About this Structure
1GSZ is a [Single protein] structure of sequence from [Alicyclobacillus acidocaldarius] with C8E and R71 as [ligands]. 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
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