1qjq

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{{STRUCTURE_1qjq| PDB=1qjq | SCENE= }}
{{STRUCTURE_1qjq| PDB=1qjq | SCENE= }}
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'''FERRIC HYDROXAMATE RECEPTOR FROM ESCHERICHIA COLI (FHUA)'''
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===FERRIC HYDROXAMATE RECEPTOR FROM ESCHERICHIA COLI (FHUA)===
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==Overview==
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One alternative method for drug delivery involves the use of siderophore-antibiotic conjugates. These compounds represent a specific means by which potent antimicrobial agents, covalently linked to iron-chelating siderophores, can be actively transported across the outer membrane of gram-negative bacteria. These "Trojan Horse" antibiotics may prove useful as an efficient means to combat multi-drug-resistant bacterial infections. Here we present the crystallographic structures of the natural siderophore-antibiotic conjugate albomycin and the siderophore phenylferricrocin, in complex with the active outer membrane transporter FhuA from Escherichia coli. To our knowledge, this represents the first structure of an antibiotic bound to its cognate transporter. Albomycins are broad-host range antibiotics that consist of a hydroxamate-type iron-chelating siderophore, and an antibiotically active, thioribosyl pyrimidine moiety. As observed with other hydroxamate-type siderophores, the three-dimensional structure of albomycin reveals an identical coordination geometry surrounding the ferric iron atom. Unexpectedly, this antibiotic assumes two conformational isomers in the binding site of FhuA, an extended and a compact form. The structural information derived from this study provides novel insights into the diverse array of antibiotic moieties that can be linked to the distal portion of iron-chelating siderophores and offers a structural platform for the rational design of hydroxamate-type siderophore-antibiotic conjugates.
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(as it appears on PubMed at http://www.pubmed.gov), where 10850805 is the PubMed ID number.
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{{ABSTRACT_PUBMED_10850805}}
==About this Structure==
==About this Structure==
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[[Category: Siderophore-antibiotic conjugate]]
[[Category: Siderophore-antibiotic conjugate]]
[[Category: Tonb-dependent receptor]]
[[Category: Tonb-dependent receptor]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 06:21:24 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 14:42:32 2008''

Revision as of 11:42, 29 July 2008

Image:1qjq.png

Template:STRUCTURE 1qjq

FERRIC HYDROXAMATE RECEPTOR FROM ESCHERICHIA COLI (FHUA)

Template:ABSTRACT PUBMED 10850805

About this Structure

1QJQ is a Single protein structure of sequence from Escherichia coli. Full crystallographic information is available from OCA.

Reference

Crystal structure of the antibiotic albomycin in complex with the outer membrane transporter FhuA., Ferguson AD, Braun V, Fiedler HP, Coulton JW, Diederichs K, Welte W, Protein Sci. 2000 May;9(5):956-63. PMID:10850805

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