2q7t

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{{STRUCTURE_2q7t| PDB=2q7t | SCENE= }}
{{STRUCTURE_2q7t| PDB=2q7t | SCENE= }}
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'''Crystal Structure of the F plasmid TraI Relaxase Domain with the Scissile Thymidine Base'''
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===Crystal Structure of the F plasmid TraI Relaxase Domain with the Scissile Thymidine Base===
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==Overview==
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Conjugative transfer of plasmid DNA via close cell-cell junctions is the main route by which antibiotic resistance genes spread between bacterial strains. Relaxases are essential for conjugative transfer and act by cleaving DNA strands and forming covalent phosphotyrosine linkages. Based on data indicating that multityrosine relaxase enzymes can accommodate two phosphotyrosine intermediates within their divalent metal-containing active sites, we hypothesized that bisphosphonates would inhibit relaxase activity and conjugative DNA transfer. We identified bisphosphonates that are nanomolar inhibitors of the F plasmid conjugative relaxase in vitro. Furthermore, we used cell-based assays to demonstrate that these compounds are highly effective at preventing DNA transfer and at selectively killing cells harboring conjugative plasmids. Two potent inhibitors, clodronate and etidronate, are already clinically approved to treat bone loss. Thus, the inhibition of conjugative relaxases is a potentially novel antimicrobial approach, one that selectively targets bacteria capable of transferring antibiotic resistance and generating multidrug resistant strains.
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==About this Structure==
==About this Structure==
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[[Category: Hydrolase]]
[[Category: Hydrolase]]
[[Category: Relaxase]]
[[Category: Relaxase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu May 22 21:35:19 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 22:28:02 2008''

Revision as of 19:28, 28 July 2008

Image:2q7t.png

Template:STRUCTURE 2q7t

Crystal Structure of the F plasmid TraI Relaxase Domain with the Scissile Thymidine Base

Template:ABSTRACT PUBMED 17630285

About this Structure

2Q7T is a Single protein structure of sequence from Escherichia coli. Full crystallographic information is available from OCA.

Reference

Disrupting antibiotic resistance propagation by inhibiting the conjugative DNA relaxase., Lujan SA, Guogas LM, Ragonese H, Matson SW, Redinbo MR, Proc Natl Acad Sci U S A. 2007 Jul 24;104(30):12282-7. Epub 2007 Jul 13. PMID:17630285

Page seeded by OCA on Mon Jul 28 22:28:02 2008

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