2aq9

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{{STRUCTURE_2aq9| PDB=2aq9 | SCENE= }}
{{STRUCTURE_2aq9| PDB=2aq9 | SCENE= }}
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'''Structure of E. coli LpxA with a bound peptide that is competitive with acyl-ACP'''
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===Structure of E. coli LpxA with a bound peptide that is competitive with acyl-ACP===
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==Overview==
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UDP-GlcNAc acyltransferase (LpxA) catalyzes the first step of lipid A biosynthesis, the transfer of the R-3-hydroxyacyl chain from R-3-hydroxyacyl acyl carrier protein (ACP) to the glucosamine 3-OH group of UDP-GlcNAc. LpxA is essential for the growth of Escherichia coli and related Gram-negative bacteria. The crystal structure of the E. coli LpxA homotrimer, determined previously at 2.6 A in the absence of substrates or inhibitors, revealed that LpxA contains an unusual, left-handed parallel beta-helix fold. We now present the crystal structure at 1.8 A resolution of E. coli LpxA in a complex with a pentadecapeptide, peptide 920. Three peptides, each of which adopts a beta-hairpin conformation, are bound per LpxA trimer. The peptides are located at the interfaces of adjacent subunits in the vicinity of the three active sites. Each peptide interacts with residues from both adjacent subunits. Peptide 920 is a potent inhibitor of E. coli LpxA (Ki = 50 nM). It is competitive with respect to acyl-ACP but not UDP-GlcNAc. The compact beta-turn structure of peptide 920 bound to LpxA may open previously uncharacterized approaches to the rational design of LpxA inhibitors with antibiotic activity.
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The line below this paragraph, {{ABSTRACT_PUBMED_16835299}}, adds the Publication Abstract to the page
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(as it appears on PubMed at http://www.pubmed.gov), where 16835299 is the PubMed ID number.
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{{ABSTRACT_PUBMED_16835299}}
==About this Structure==
==About this Structure==
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[[Category: Peptide inhibitor]]
[[Category: Peptide inhibitor]]
[[Category: Udp-glcnac]]
[[Category: Udp-glcnac]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 19:20:29 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 03:20:07 2008''

Revision as of 00:20, 29 July 2008

Image:2aq9.png

Template:STRUCTURE 2aq9

Structure of E. coli LpxA with a bound peptide that is competitive with acyl-ACP

Template:ABSTRACT PUBMED 16835299

About this Structure

2AQ9 is a Single protein structure of sequence from Escherichia coli. Full crystallographic information is available from OCA.

Reference

Structure of UDP-N-acetylglucosamine acyltransferase with a bound antibacterial pentadecapeptide., Williams AH, Immormino RM, Gewirth DT, Raetz CR, Proc Natl Acad Sci U S A. 2006 Jul 18;103(29):10877-82. Epub 2006 Jul 11. PMID:16835299

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