2f9a

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Revision as of 17:31, 29 January 2008

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spinqualitylabelsall models 2f9a, resolution 2.51Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image

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

Overview

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.

About this Structure

2F9A is a Single protein structure of sequence from Brassica juncea with as ligand. 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

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