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2gkl

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{{STRUCTURE_2gkl| PDB=2gkl | SCENE= }}
{{STRUCTURE_2gkl| PDB=2gkl | SCENE= }}
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'''Crystal structure of the zinc carbapenemase CPHA in complex with the inhibitor pyridine-2,4-dicarboxylate'''
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===Crystal structure of the zinc carbapenemase CPHA in complex with the inhibitor pyridine-2,4-dicarboxylate===
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==Overview==
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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.
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The line below this paragraph, {{ABSTRACT_PUBMED_17307979}}, adds the Publication Abstract to the page
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(as it appears on PubMed at http://www.pubmed.gov), where 17307979 is the PubMed ID number.
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{{ABSTRACT_PUBMED_17307979}}
==About this Structure==
==About this Structure==
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==Reference==
==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:[http://www.ncbi.nlm.nih.gov/pubmed/17307979 17307979]
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:[http://www.ncbi.nlm.nih.gov/pubmed/17307979 17307979]
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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:[http://www.ncbi.nlm.nih.gov/pubmed/15588826 15588826]
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Update of the standard numbering scheme for class B beta-lactamases., Garau G, Garcia-Saez I, Bebrone C, Anne C, Mercuri P, Galleni M, Frere JM, Dideberg O, Antimicrob Agents Chemother. 2004 Jul;48(7):2347-9. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/15215079 15215079]
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The 3-D structure of a zinc metallo-beta-lactamase from Bacillus cereus reveals a new type of protein fold., Carfi A, Pares S, Duee E, Galleni M, Duez C, Frere JM, Dideberg O, EMBO J. 1995 Oct 16;14(20):4914-21. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/7588620 7588620]
[[Category: Aeromonas hydrophila]]
[[Category: Aeromonas hydrophila]]
[[Category: Beta-lactamase]]
[[Category: Beta-lactamase]]
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[[Category: Lactamase]]
[[Category: Lactamase]]
[[Category: Zn]]
[[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 Jul 28 21:24:53 2008''

Revision as of 18:25, 28 July 2008

Image:2gkl.png

Template:STRUCTURE 2gkl

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

Template:ABSTRACT PUBMED 17307979

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

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

Update of the standard numbering scheme for class B beta-lactamases., Garau G, Garcia-Saez I, Bebrone C, Anne C, Mercuri P, Galleni M, Frere JM, Dideberg O, Antimicrob Agents Chemother. 2004 Jul;48(7):2347-9. PMID:15215079

The 3-D structure of a zinc metallo-beta-lactamase from Bacillus cereus reveals a new type of protein fold., Carfi A, Pares S, Duee E, Galleni M, Duez C, Frere JM, Dideberg O, EMBO J. 1995 Oct 16;14(20):4914-21. PMID:7588620

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