2fa0
From Proteopedia
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|PDB= 2fa0 |SIZE=350|CAPTION= <scene name='initialview01'>2fa0</scene>, resolution 2.49Å | |PDB= 2fa0 |SIZE=350|CAPTION= <scene name='initialview01'>2fa0</scene>, resolution 2.49Å | ||
|SITE= | |SITE= | ||
| - | |LIGAND= <scene name='pdbligand=HMG:3-HYDROXY-3-METHYLGLUTARYL-COENZYME A'>HMG</scene> | + | |LIGAND= <scene name='pdbligand=HMG:3-HYDROXY-3-METHYLGLUTARYL-COENZYME+A'>HMG</scene> |
|ACTIVITY= | |ACTIVITY= | ||
|GENE= | |GENE= | ||
| + | |DOMAIN= | ||
| + | |RELATEDENTRY=[[2f82|2F82]], [[2f9a|2F9A]], [[2fa3|2FA3]] | ||
| + | |RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2fa0 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2fa0 OCA], [http://www.ebi.ac.uk/pdbsum/2fa0 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2fa0 RCSB]</span> | ||
}} | }} | ||
| Line 26: | Line 29: | ||
[[Category: Pojer, F.]] | [[Category: Pojer, F.]] | ||
[[Category: Richard, S B.]] | [[Category: Richard, S B.]] | ||
| - | [[Category: HMG]] | ||
[[Category: hmg-coa]] | [[Category: hmg-coa]] | ||
[[Category: hmgs1]] | [[Category: hmgs1]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 02:59:58 2008'' |
Revision as of 00:00, 31 March 2008
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| , resolution 2.49Å | |||||||
|---|---|---|---|---|---|---|---|
| Ligands: | |||||||
| Related: | 2F82, 2F9A, 2FA3
| ||||||
| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
HMG-CoA synthase from Brassica juncea in complex with HMG-CoA and covalently bound to HMG-CoA
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
2FA0 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
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