1x8i

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[[Image:1x8i.jpg|left|200px]]
[[Image:1x8i.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 1x8i |SIZE=350|CAPTION= <scene name='initialview01'>1x8i</scene>, resolution 1.90&Aring;
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The line below this paragraph, containing "STRUCTURE_1x8i", 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=BMH:5H-PYRAZOLO(1,2-A)(1,2,4)TRIAZOL-4-IUM,+6-((2-CARBOXY-6-(1-HYDROXYETHYL)-4-METHYL-7-OXO-1-AZABICYCLO(3.2.0)HEPT-2-EN-3-YL)THIO)-6,7-DIHYDRO-,+HYDROXIDE,+INNER+SALT,+(4R-(4ALPHA,5BETA,6BETA(R*)))-'>BMH</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</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= cphA ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=644 Aeromonas hydrophila])
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-->
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|DOMAIN=
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{{STRUCTURE_1x8i| PDB=1x8i | SCENE= }}
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|RELATEDENTRY=[[1x8g|1X8G]], [[1x8h|1X8H]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1x8i FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1x8i OCA], [http://www.ebi.ac.uk/pdbsum/1x8i PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1x8i RCSB]</span>
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}}
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'''Crystal Structure of the Zinc Carbapenemase CphA in Complex with the Antibiotic Biapenem'''
'''Crystal Structure of the Zinc Carbapenemase CphA in Complex with the Antibiotic Biapenem'''
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[[Category: Dideberg, O.]]
[[Category: Dideberg, O.]]
[[Category: Garau, G.]]
[[Category: Garau, G.]]
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[[Category: hydrolase]]
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[[Category: Hydrolase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 14:42:18 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 00:46:09 2008''
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Revision as of 11:42, 3 May 2008

Image:1x8i.jpg

Template:STRUCTURE 1x8i

Crystal Structure of the Zinc Carbapenemase CphA in Complex with the Antibiotic Biapenem


Overview

One strategy developed by bacteria to resist the action of beta-lactam antibiotics is the expression of metallo-beta-lactamases. CphA from Aeromonas hydrophila is a member of a clinically important subclass of metallo-beta-lactamases that have only one zinc ion in their active site and for which no structure is available. The crystal structures of wild-type CphA and its N220G mutant show the structural features of the active site of this enzyme, which is modeled specifically for carbapenem hydrolysis. The structure of CphA after reaction with a carbapenem substrate, biapenem, reveals that the enzyme traps a reaction intermediate in the active site. These three X-ray structures have allowed us to propose how the enzyme recognizes carbapenems and suggest a mechanistic pathway for hydrolysis of the beta-lactam. This will be relevant for the design of metallo-beta-lactamase inhibitors as well as of antibiotics that escape their hydrolytic activity.

About this Structure

1X8I is a Single protein structure of sequence from Aeromonas hydrophila. Full crystallographic information is available from OCA.

Reference

A metallo-beta-lactamase enzyme in action: crystal structures of the monozinc carbapenemase CphA and its complex with biapenem., Garau G, Bebrone C, Anne C, Galleni M, Frere JM, Dideberg O, J Mol Biol. 2005 Jan 28;345(4):785-95. PMID:15588826 Page seeded by OCA on Sat May 3 14:42:18 2008

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