2qdt

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[[Image:2qdt.jpg|left|200px]]
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{{Seed}}
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{{STRUCTURE_2qdt| PDB=2qdt | SCENE= }}
{{STRUCTURE_2qdt| PDB=2qdt | SCENE= }}
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'''Structural Basis for the Broad-Spectrum Inhibition of Metallo-{Beta}-Lactamases: L1- IS38 Complex'''
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===Structural Basis for the Broad-Spectrum Inhibition of Metallo-{Beta}-Lactamases: L1- IS38 Complex===
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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_18563261}}, adds the Publication Abstract to the page
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(as it appears on PubMed at http://www.pubmed.gov), where 18563261 is the PubMed ID number.
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{{ABSTRACT_PUBMED_18563261}}
==About this Structure==
==About this Structure==
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==Reference==
==Reference==
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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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Structural basis for the broad-spectrum inhibition of metallo-beta-lactamases by thiols., Lienard BM, Garau G, Horsfall L, Karsisiotis AI, Damblon C, Lassaux P, Papamicael C, Roberts GC, Galleni M, Dideberg O, Frere JM, Schofield CJ, Org Biomol Chem. 2008 Jul 7;6(13):2282-94. Epub 2008 May 7. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/18563261 18563261]
[[Category: Beta-lactamase]]
[[Category: Beta-lactamase]]
[[Category: Single protein]]
[[Category: Single protein]]
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[[Category: Metallo]]
[[Category: Metallo]]
[[Category: Zn]]
[[Category: Zn]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 14:47:09 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jul 9 10:07:06 2008''

Revision as of 07:07, 9 July 2008

Image:2qdt.png

Template:STRUCTURE 2qdt

Structural Basis for the Broad-Spectrum Inhibition of Metallo-{Beta}-Lactamases: L1- IS38 Complex

Template:ABSTRACT PUBMED 18563261

About this Structure

2QDT is a Single protein structure of sequence from Stenotrophomonas maltophilia. Full crystallographic information is available from OCA.

Reference

Structural basis for the broad-spectrum inhibition of metallo-beta-lactamases by thiols., Lienard BM, Garau G, Horsfall L, Karsisiotis AI, Damblon C, Lassaux P, Papamicael C, Roberts GC, Galleni M, Dideberg O, Frere JM, Schofield CJ, Org Biomol Chem. 2008 Jul 7;6(13):2282-94. Epub 2008 May 7. PMID:18563261

Page seeded by OCA on Wed Jul 9 10:07:06 2008

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