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2f9a

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[[Image:2f9a.gif|left|200px]]
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{{Seed}}
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[[Image:2f9a.png|left|200px]]
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{{STRUCTURE_2f9a| PDB=2f9a | SCENE= }}
{{STRUCTURE_2f9a| PDB=2f9a | SCENE= }}
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'''HMG-CoA synthase from Brassica juncea in complex with F-244'''
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===HMG-CoA synthase from Brassica juncea in complex with F-244===
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==Overview==
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3-Hydroxy-3-methylglutaryl CoA synthase (HMGS) catalyzes the first committed step in the mevalonate metabolic pathway for isoprenoid biosynthesis and serves as an alternative target for cholesterol-lowering and antibiotic drugs. We have determined a previously undescribed crystal structure of a eukaryotic HMGS bound covalently to a potent and specific inhibitor F-244 [(E,E)-11-[3-(hydroxymethyl)-4-oxo-2-oxytanyl]-3,5,7-trimethyl-2,4-undecad ienenoic acid]. Given the accessibility of synthetic analogs of the F-244 natural product, this inhibited eukaryotic HMGS structure serves as a necessary starting point for structure-based methods that may improve the potency and species-specific selectivity of the next generation of F-244 analogs designed to target particular eukaryotic and prokaryotic HMGS.
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The line below this paragraph, {{ABSTRACT_PUBMED_16864776}}, adds the Publication Abstract to the page
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(as it appears on PubMed at http://www.pubmed.gov), where 16864776 is the PubMed ID number.
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{{ABSTRACT_PUBMED_16864776}}
==About this Structure==
==About this Structure==
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[[Category: F-244]]
[[Category: F-244]]
[[Category: Hmgs1]]
[[Category: Hmgs1]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 03:37:06 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Jul 27 20:14:42 2008''

Revision as of 17:14, 27 July 2008

Image:2f9a.png

Template:STRUCTURE 2f9a

HMG-CoA synthase from Brassica juncea in complex with F-244

Template:ABSTRACT PUBMED 16864776

About this Structure

2F9A is a Single protein structure of sequence from Brassica juncea. Full crystallographic information is available from OCA.

Reference

Structural basis for the design of potent and species-specific inhibitors of 3-hydroxy-3-methylglutaryl CoA synthases., Pojer F, Ferrer JL, Richard SB, Nagegowda DA, Chye ML, Bach TJ, Noel JP, Proc Natl Acad Sci U S A. 2006 Aug 1;103(31):11491-6. Epub 2006 Jul 24. PMID:16864776

Page seeded by OCA on Sun Jul 27 20:14:42 2008

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