2gkl

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[[Image:2gkl.jpg|left|200px]]
[[Image:2gkl.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 2gkl |SIZE=350|CAPTION= <scene name='initialview01'>2gkl</scene>, resolution 1.86&Aring;
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The line below this paragraph, containing "STRUCTURE_2gkl", 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=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=PD2:PYRIDINE-2,4-DICARBOXYLIC+ACID'>PD2</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_2gkl| PDB=2gkl | SCENE= }}
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|RELATEDENTRY=[[1x8i|1X8I]], [[1x8h|1X8H]], [[1x8g|1X8G]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2gkl FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2gkl OCA], [http://www.ebi.ac.uk/pdbsum/2gkl PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2gkl RCSB]</span>
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}}
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'''Crystal structure of the zinc carbapenemase CPHA in complex with the inhibitor pyridine-2,4-dicarboxylate'''
'''Crystal structure of the zinc carbapenemase CPHA in complex with the inhibitor pyridine-2,4-dicarboxylate'''
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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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[[Category: inhibitor]]
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[[Category: Inhibitor]]
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[[Category: lactamase]]
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[[Category: Lactamase]]
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[[Category: zn]]
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[[Category: Zn]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 05:12:37 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 03:17:52 2008''
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Revision as of 02:12, 4 May 2008

Image:2gkl.jpg

Template:STRUCTURE 2gkl

Crystal structure of the zinc carbapenemase CPHA in complex with the inhibitor pyridine-2,4-dicarboxylate


Overview

Various inhibitors of metallo-beta-lactamases have been reported; however, none are effective for all subgroups. Those that have been found to inhibit the enzymes of subclass B2 (catalytically active with one zinc) either contain a thiol (and show less inhibition towards this subgroup than towards the dizinc members of B1 and B3) or are inactivators behaving as substrates for the dizinc family members. The present work reveals that certain pyridine carboxylates are competitive inhibitors of CphA, a subclass B2 enzyme. X-ray crystallographic analyses demonstrate that pyridine-2,4-dicarboxylic acid chelates the zinc ion in a bidentate manner within the active site. Salts of these compounds are already available and undergoing biomedical testing for various nonrelated purposes. Pyridine carboxylates appear to be useful templates for the development of more-complex, selective, nontoxic inhibitors of subclass B2 metallo-beta-lactamases.

About this Structure

2GKL is a Single protein structure of sequence from Aeromonas hydrophila. Full crystallographic information is available from OCA.

Reference

Competitive inhibitors of the CphA metallo-beta-lactamase from Aeromonas hydrophila., Horsfall LE, Garau G, Lienard BM, Dideberg O, Schofield CJ, Frere JM, Galleni M, Antimicrob Agents Chemother. 2007 Jun;51(6):2136-42. Epub 2007 Feb 16. PMID:17307979 Page seeded by OCA on Sun May 4 05:12:37 2008

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