This old version of Proteopedia is provided for student assignments while the new version is undergoing repairs. Content and edits done in this old version of Proteopedia after March 1, 2026 will eventually be lost when it is retired in about June of 2026.
Apply for new accounts at the new Proteopedia. Your logins will work in both the old and new versions.
2fa0
From Proteopedia
| Line 4: | Line 4: | ||
|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
| |||||||
| , 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
Page seeded by OCA on Mon Mar 31 02:59:58 2008
