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| ==Crystal structure of CviR bound to antagonist chlorolactone (CL)== | | ==Crystal structure of CviR bound to antagonist chlorolactone (CL)== |
| <StructureSection load='3qp5' size='340' side='right' caption='[[3qp5]], [[Resolution|resolution]] 3.25Å' scene=''> | | <StructureSection load='3qp5' size='340' side='right'caption='[[3qp5]], [[Resolution|resolution]] 3.25Å' scene=''> |
| == Structural highlights == | | == Structural highlights == |
| <table><tr><td colspan='2'>[[3qp5]] is a 4 chain structure with sequence from [http://en.wikipedia.org/wiki/Chromobacterium_violaceum Chromobacterium violaceum]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3QP5 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3QP5 FirstGlance]. <br> | | <table><tr><td colspan='2'>[[3qp5]] is a 4 chain structure with sequence from [https://en.wikipedia.org/wiki/Chromobacterium_violaceum Chromobacterium violaceum]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3QP5 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3QP5 FirstGlance]. <br> |
| </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=HLC:4-(4-CHLOROPHENOXY)-N-[(3S)-2-OXOTETRAHYDROFURAN-3-YL]BUTANAMIDE'>HLC</scene></td></tr> | | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 3.249Å</td></tr> |
| <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[3qp1|3qp1]], [[3qp2|3qp2]], [[3qp4|3qp4]], [[3qp6|3qp6]], [[3qp7|3qp7]], [[3qp8|3qp8]]</td></tr> | | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=HLC:4-(4-CHLOROPHENOXY)-N-[(3S)-2-OXOTETRAHYDROFURAN-3-YL]BUTANAMIDE'>HLC</scene></td></tr> |
| <tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">cviR ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=536 Chromobacterium violaceum])</td></tr>
| | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=3qp5 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3qp5 OCA], [https://pdbe.org/3qp5 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3qp5 RCSB], [https://www.ebi.ac.uk/pdbsum/3qp5 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3qp5 ProSAT]</span></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=3qp5 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3qp5 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3qp5 RCSB], [http://www.ebi.ac.uk/pdbsum/3qp5 PDBsum]</span></td></tr> | |
| </table> | | </table> |
| <div style="background-color:#fffaf0;">
| | == Function == |
| == Publication Abstract from PubMed == | | [https://www.uniprot.org/uniprot/D3W065_CHRVL D3W065_CHRVL] |
| Quorum-sensing bacteria communicate via small molecules called autoinducers to coordinate collective behaviors. Because quorum sensing controls virulence factor expression in many clinically relevant pathogens, membrane-permeable quorum sensing antagonists that prevent population-wide expression of virulence genes offer a potential route to novel antibacterial therapeutics. Here, we report a strategy for inhibiting quorum-sensing receptors of the widespread LuxR family. Structure-function studies with natural and synthetic ligands demonstrate that the dimeric LuxR-type transcription factor CviR from Chromobacterium violaceum is potently antagonized by molecules that bind in place of the native acylated homoserine lactone autoinducer, provided that they stabilize a closed conformation. In such conformations, each of the two DNA-binding domains interacts with the ligand-binding domain of the opposing monomer. Consequently, the DNA-binding helices are held apart by approximately 60 A, twice the approximately 30 A separation required for operator binding. This approach may represent a general strategy for the inhibition of multidomain proteins.
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| A strategy for antagonizing quorum sensing.,Chen G, Swem LR, Swem DL, Stauff DL, O'Loughlin CT, Jeffrey PD, Bassler BL, Hughson FM Mol Cell. 2011 Apr 22;42(2):199-209. PMID:21504831<ref>PMID:21504831</ref>
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| From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
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| </div>
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| == References ==
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| <references/>
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| __TOC__ | | __TOC__ |
| </StructureSection> | | </StructureSection> |
| [[Category: Chromobacterium violaceum]] | | [[Category: Chromobacterium violaceum]] |
| [[Category: Bassler, B]] | | [[Category: Large Structures]] |
| [[Category: Chen, G]] | | [[Category: Bassler B]] |
| [[Category: Hughson, F]] | | [[Category: Chen G]] |
| [[Category: Jeffrey, P]] | | [[Category: Hughson F]] |
| [[Category: Loughlin, C O]] | | [[Category: Jeffrey P]] |
| [[Category: Stauff, D]] | | [[Category: O'Loughlin C]] |
| [[Category: Swem, D]] | | [[Category: Stauff D]] |
| [[Category: Swem, L]] | | [[Category: Swem D]] |
| [[Category: Acylated homoserine lactone]]
| | [[Category: Swem L]] |
| [[Category: Agonist]]
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| [[Category: Antagonist]]
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| [[Category: Dna binding protein]]
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| [[Category: Ligand binding domain]]
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| [[Category: Luxr]]
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| [[Category: Quorum sensing]]
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| [[Category: Quorum sensing transcription factor]]
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| [[Category: Signal receptor]]
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| [[Category: Transcription]]
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| [[Category: Transcription factor]]
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