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| [[Image:1p42.gif|left|200px]] | | {{Seed}} |
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| {{STRUCTURE_1p42| PDB=1p42 | SCENE= }} | | {{STRUCTURE_1p42| PDB=1p42 | SCENE= }} |
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| '''Crystal structure of Aquifex aeolicus LpxC Deacetylase (Zinc-Inhibited Form)'''
| | ===Crystal structure of Aquifex aeolicus LpxC Deacetylase (Zinc-Inhibited Form)=== |
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| ==Overview==
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| The outer leaflet of the outer membrane of the Gram-negative bacterium serves as a permeability barrier and is composed of lipopolysaccharide, also known as endotoxin. The membrane anchor of lipopolysaccharide is lipid A, the biosynthesis of which is essential for cell viability. The first committed step in lipid A biosynthesis is catalyzed by UDP-(3-O-(R-3-hydroxymyristoyl))-N-acetylglucosamine deacetylase (LpxC), a zinc-dependent deacetylase. Here we report the crystal structure of LpxC from Aquifex aeolicus, which reveals a new alpha+beta fold reflecting primordial gene duplication and fusion, as well as a new zinc-binding motif. The catalytic zinc ion resides at the base of an active-site cleft and adjacent to a hydrophobic tunnel occupied by a fatty acid. This tunnel accounts for the specificity of LpxC toward substrates and inhibitors bearing appropriately positioned 3-O-fatty acid substituents. Notably, simple inhibitors designed to target interactions in the hydrophobic tunnel bind with micromolar affinity, thereby representing a step toward the structure-based design of a potent, broad-spectrum antibacterial drug. | | The line below this paragraph, {{ABSTRACT_PUBMED_12819349}}, adds the Publication Abstract to the page |
| | (as it appears on PubMed at http://www.pubmed.gov), where 12819349 is the PubMed ID number. |
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| | {{ABSTRACT_PUBMED_12819349}} |
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| ==About this Structure== | | ==About this Structure== |
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| [[Category: Alpha+beta fold]] | | [[Category: Alpha+beta fold]] |
| [[Category: Hydrophobic tunnel]] | | [[Category: Hydrophobic tunnel]] |
| ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 04:39:20 2008'' | | |
| | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 17:27:30 2008'' |
