1a8t

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[[Image:1a8t.gif|left|200px]]
[[Image:1a8t.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 1a8t |SIZE=350|CAPTION= <scene name='initialview01'>1a8t</scene>, resolution 2.55&Aring;
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The line below this paragraph, containing "STRUCTURE_1a8t", creates the "Structure Box" on the page.
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|SITE=
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=061:2-BUTYL-6-HYDROXY-3-[2&#39;-(1H-TETRAZOL-5-YL)-BIPHENYL-4-YLMETHYL]-3H-QUINAZOLIN-4-ONE'>061</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY= <span class='plainlinks'>[http://en.wikipedia.org/wiki/Beta-lactamase Beta-lactamase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.5.2.6 3.5.2.6] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE= CCRA ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=817 Bacteroides fragilis])
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-->
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|DOMAIN=
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{{STRUCTURE_1a8t| PDB=1a8t | SCENE= }}
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|RELATEDENTRY=
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1a8t FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1a8t OCA], [http://www.ebi.ac.uk/pdbsum/1a8t PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1a8t RCSB]</span>
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}}
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'''METALLO-BETA-LACTAMASE IN COMPLEX WITH L-159,061'''
'''METALLO-BETA-LACTAMASE IN COMPLEX WITH L-159,061'''
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[[Category: Toney, J H.]]
[[Category: Toney, J H.]]
[[Category: Vanderwall, D.]]
[[Category: Vanderwall, D.]]
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[[Category: antibiotic resistance]]
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[[Category: Antibiotic resistance]]
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[[Category: beta-lactamase]]
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[[Category: Beta-lactamase]]
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[[Category: hydrolase]]
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[[Category: Hydrolase]]
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[[Category: metallo-beta-lactamase]]
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[[Category: Metallo-beta-lactamase]]
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[[Category: zinc]]
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[[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 Sun Mar 30 18:35:42 2008''
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Revision as of 06:59, 2 May 2008

Image:1a8t.gif

Template:STRUCTURE 1a8t

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


Overview

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.

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 Fri May 2 09:59:22 2008

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OCA

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