1a8t

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{{STRUCTURE_1a8t| PDB=1a8t | SCENE= }}
{{STRUCTURE_1a8t| PDB=1a8t | SCENE= }}
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'''METALLO-BETA-LACTAMASE IN COMPLEX WITH L-159,061'''
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===METALLO-BETA-LACTAMASE IN COMPLEX WITH L-159,061===
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==Overview==
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BACKGROUND: High level resistance to carbapenem antibiotics in gram negative bacteria such as Bacteroides fragilis is caused, in part, by expression of a wide-spectrum metallo-beta-lactamase that hydrolyzes the drug to an inactive form. Co-administration of metallo-beta-lactamase inhibitors to resistant bacteria is expected to restore the antibacterial activity of carbapenems. RESULTS: Biphenyl tetrazoles (BPTs) are a structural class of potent competitive inhibitors of metallo-beta-lactamase identified through screening and predicted using molecular modeling of the enzyme structure. The X-ray crystal structure of the enzyme bound to the BPT L-159,061 shows that the tetrazole moiety of the inhibitor interacts directly with one of the two zinc atoms in the active site, replacing a metal-bound water molecule. Inhibition of metallo-beta-lactamase by BPTs in vitro correlates well with antibiotic sensitization of resistant B. fragilis. CONCLUSIONS: BPT inhibitors can sensitize a resistant B. fragilis clinical isolate expressing metallo-beta-lactamase to the antibiotics imipenem or penicillin G but not to rifampicin.
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(as it appears on PubMed at http://www.pubmed.gov), where 9545432 is the PubMed ID number.
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{{ABSTRACT_PUBMED_9545432}}
==About this Structure==
==About this Structure==
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[[Category: Metallo-beta-lactamase]]
[[Category: Metallo-beta-lactamase]]
[[Category: Zinc]]
[[Category: Zinc]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 09:59:22 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jun 30 16:23:49 2008''

Revision as of 13:23, 30 June 2008

Image:1a8t.png

Template:STRUCTURE 1a8t

METALLO-BETA-LACTAMASE IN COMPLEX WITH L-159,061

Template:ABSTRACT PUBMED 9545432

About this Structure

1A8T is a Single protein structure of sequence from Bacteroides fragilis. Full crystallographic information is available from OCA.

Reference

Antibiotic sensitization using biphenyl tetrazoles as potent inhibitors of Bacteroides fragilis metallo-beta-lactamase., Toney JH, Fitzgerald PM, Grover-Sharma N, Olson SH, May WJ, Sundelof JG, Vanderwall DE, Cleary KA, Grant SK, Wu JK, Kozarich JW, Pompliano DL, Hammond GG, Chem Biol. 1998 Apr;5(4):185-96. PMID:9545432

Page seeded by OCA on Mon Jun 30 16:23:49 2008

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