2ves

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{{STRUCTURE_2ves| PDB=2ves | SCENE= }}
{{STRUCTURE_2ves| PDB=2ves | SCENE= }}
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'''CRYSTAL STRUCTURE OF LPXC FROM PSEUDOMONAS AERUGINOSA COMPLEXED WITH THE POTENT BB-78485 INHIBITOR'''
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===CRYSTAL STRUCTURE OF LPXC FROM PSEUDOMONAS AERUGINOSA COMPLEXED WITH THE POTENT BB-78485 INHIBITOR===
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==Overview==
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The cell wall in Gram-negative bacteria is surrounded by an outer membrane comprised of charged lipopolysaccharide (LPS) molecules that prevent entry of hydrophobic agents into the cell and protect the bacterium from many antibiotics. The hydrophobic anchor of LPS is lipid A, the biosynthesis of which is essential for bacterial growth and viability. UDP-3-O-(R-3-hydroxymyristoyl)-N-acetylglucosamine deacetylase (LpxC) is an essential zinc-dependant enzyme that catalyzes the conversion of UDP-3-O-(R-3-hydroxymyristoyl)-N-acetylglucosamine to UDP-3-O-(R-3-hydroxymyristoyl)glucosamine and acetate in the biosynthesis of lipid A, and for this reason, LpxC is an attractive target for antibacterial drug discovery. Here we disclose a 1.9 A resolution crystal structure of LpxC from Pseudomonas aeruginosa (paLpxC) in a complex with the potent BB-78485 inhibitor. To our knowledge, this is the first crystal structure of LpxC with a small-molecule inhibitor that shows antibacterial activity against a wide range of Gram-negative pathogens. Accordingly, this structure can provide important information for lead optimization and rational design of the effective small-molecule LpxC inhibitors for successful treatment of Gram-negative infections.
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{{ABSTRACT_PUBMED_18287278}}
==About this Structure==
==About this Structure==
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[[Category: Lpxc]]
[[Category: Lpxc]]
[[Category: Metalloprotease]]
[[Category: Metalloprotease]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 18:40:59 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 00:53:47 2008''

Revision as of 21:53, 27 July 2008

Image:2ves.png

Template:STRUCTURE 2ves

CRYSTAL STRUCTURE OF LPXC FROM PSEUDOMONAS AERUGINOSA COMPLEXED WITH THE POTENT BB-78485 INHIBITOR

Template:ABSTRACT PUBMED 18287278

About this Structure

2VES is a Single protein structure of sequence from Pseudomonas aeruginosa. Full crystallographic information is available from OCA.

Reference

Crystal structure of LpxC from Pseudomonas aeruginosa complexed with the potent BB-78485 inhibitor., Mochalkin I, Knafels JD, Lightle S, Protein Sci. 2008 Mar;17(3):450-7. PMID:18287278

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