4yx9: Difference between revisions
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''' | ==Crystal structure of the CFTR inhibitory factor Cif bound to tiratricol== | ||
<StructureSection load='4yx9' size='340' side='right' caption='[[4yx9]], [[Resolution|resolution]] 1.75Å' scene=''> | |||
== Structural highlights == | |||
<table><tr><td colspan='2'>[[4yx9]] is a 4 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4YX9 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4YX9 FirstGlance]. <br> | |||
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=4HY:[4-(4-HYDROXY-3-IODO-PHENOXY)-3,5-DIIODO-PHENYL]-ACETIC+ACID'>4HY</scene></td></tr> | |||
<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[3kd2|3kd2]]</td></tr> | |||
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4yx9 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4yx9 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4yx9 RCSB], [http://www.ebi.ac.uk/pdbsum/4yx9 PDBsum]</span></td></tr> | |||
</table> | |||
<div style="background-color:#fffaf0;"> | |||
== Publication Abstract from PubMed == | |||
Opportunistic pathogens exploit diverse strategies to sabotage host defenses. Pseudomonas aeruginosa secretes the CFTR inhibitory factor Cif and thus triggers loss of CFTR, an ion channel required for airway mucociliary defense. However, the mechanism of action of Cif has remained unclear. It catalyzes epoxide hydrolysis, but there is no known role for natural epoxides in CFTR regulation. It was demonstrated that the hydrolase activity of Cif is strictly required for its effects on CFTR. A small-molecule inhibitor that protects this key component of the mucociliary defense system was also uncovered. These results provide a basis for targeting the distinctive virulence chemistry of Cif and suggest an unanticipated role of physiological epoxides in intracellular protein trafficking. | |||
Inhibiting an epoxide hydrolase virulence factor from Pseudomonas aeruginosa protects CFTR.,Bahl CD, Hvorecny KL, Bomberger JM, Stanton BA, Hammock BD, Morisseau C, Madden DR Angew Chem Int Ed Engl. 2015 Jul 1. doi: 10.1002/anie.201503983. PMID:26136396<ref>PMID:26136396</ref> | |||
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |||
</div> | |||
== References == | |||
[[Category: | <references/> | ||
[[Category: | __TOC__ | ||
[[Category: | </StructureSection> | ||
[[Category: Bahl, C D]] | |||
[[Category: Madden, D R]] | |||
[[Category: Alpha beta hydrolase]] | |||
[[Category: Cftr]] | |||
[[Category: Cif]] | |||
[[Category: Enzyme]] | |||
[[Category: Epoxide hydrolase]] | |||
[[Category: Hydrolase-hydrolase inhibitor complex]] | |||
[[Category: Inhibitor]] | |||
Revision as of 16:18, 15 July 2015
Crystal structure of the CFTR inhibitory factor Cif bound to tiratricolCrystal structure of the CFTR inhibitory factor Cif bound to tiratricol
Structural highlights
Publication Abstract from PubMedOpportunistic pathogens exploit diverse strategies to sabotage host defenses. Pseudomonas aeruginosa secretes the CFTR inhibitory factor Cif and thus triggers loss of CFTR, an ion channel required for airway mucociliary defense. However, the mechanism of action of Cif has remained unclear. It catalyzes epoxide hydrolysis, but there is no known role for natural epoxides in CFTR regulation. It was demonstrated that the hydrolase activity of Cif is strictly required for its effects on CFTR. A small-molecule inhibitor that protects this key component of the mucociliary defense system was also uncovered. These results provide a basis for targeting the distinctive virulence chemistry of Cif and suggest an unanticipated role of physiological epoxides in intracellular protein trafficking. Inhibiting an epoxide hydrolase virulence factor from Pseudomonas aeruginosa protects CFTR.,Bahl CD, Hvorecny KL, Bomberger JM, Stanton BA, Hammock BD, Morisseau C, Madden DR Angew Chem Int Ed Engl. 2015 Jul 1. doi: 10.1002/anie.201503983. PMID:26136396[1] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. References
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