6d6d

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==The structure of ligand binding domain of LasR in complex with TP-1 homolog, compound 13==
==The structure of ligand binding domain of LasR in complex with TP-1 homolog, compound 13==
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<StructureSection load='6d6d' size='340' side='right' caption='[[6d6d]], [[Resolution|resolution]] 1.70&Aring;' scene=''>
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<StructureSection load='6d6d' size='340' side='right'caption='[[6d6d]], [[Resolution|resolution]] 1.70&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>[[6d6d]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Pseae Pseae]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6D6D OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6D6D FirstGlance]. <br>
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<table><tr><td colspan='2'>[[6d6d]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Pseudomonas_aeruginosa_PAO1 Pseudomonas aeruginosa PAO1]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6D6D OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=6D6D FirstGlance]. <br>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=FY7:2,4-dibromo-6-{[(2-nitrobenzene-1-carbonyl)amino]methyl}phenyl+2-cyanobenzoate'>FY7</scene></td></tr>
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</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.7&#8491;</td></tr>
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<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[6d6a|6d6a]], [[6d6b|6d6b]], [[6d6c|6d6c]]</td></tr>
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=FY7:2,4-dibromo-6-{[(2-nitrobenzene-1-carbonyl)amino]methyl}phenyl+2-cyanobenzoate'>FY7</scene></td></tr>
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<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">lasR, PA1430 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=208964 PSEAE])</td></tr>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=6d6d FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6d6d OCA], [https://pdbe.org/6d6d PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=6d6d RCSB], [https://www.ebi.ac.uk/pdbsum/6d6d PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=6d6d ProSAT]</span></td></tr>
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<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=6d6d FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6d6d OCA], [http://pdbe.org/6d6d PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6d6d RCSB], [http://www.ebi.ac.uk/pdbsum/6d6d PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6d6d ProSAT]</span></td></tr>
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</table>
</table>
== Function ==
== Function ==
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[[http://www.uniprot.org/uniprot/LASR_PSEAE LASR_PSEAE]] Transcriptional activator of elastase structural gene (LasB). Binds to the PAI autoinducer.
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[https://www.uniprot.org/uniprot/LASR_PSEAE LASR_PSEAE] Transcriptional activator of elastase structural gene (LasB). Binds to the PAI autoinducer.
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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Chemical strategies to block quorum sensing (QS) could provide a route to attenuate virulence in bacterial pathogens. Considerable research has focused on this approach in Pseudomonas aeruginosa, which uses the LuxR-type receptor LasR to regulate much of its QS network. Non-native ligands that antagonize LasR have been developed, yet we have little understanding of the mode by which these compounds interact with LasR and alter its function, as the receptor is unstable in their presence. Herein, we report an approach to circumvent this challenge through the study of a series of synthetic LasR agonists with varying levels of potency. Structural investigations of these ligands with the LasR ligand-binding domain reveal that certain agonists can enforce a conformation that deviates from that observed for other, often more potent agonists. These results, when combined with cell-based and biophysical analyses, suggest a functional model for LasR that could guide future ligand design.
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Structural and Biochemical Studies of Non-native Agonists of the LasR Quorum-Sensing Receptor Reveal an L3 Loop "Out" Conformation for LasR.,O'Reilly MC, Dong SH, Rossi FM, Karlen KM, Kumar RS, Nair SK, Blackwell HE Cell Chem Biol. 2018 Jul 11. pii: S2451-9456(18)30221-6. doi:, 10.1016/j.chembiol.2018.06.007. PMID:30033130<ref>PMID:30033130</ref>
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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</div>
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<div class="pdbe-citations 6d6d" style="background-color:#fffaf0;"></div>
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==See Also==
==See Also==
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*[[Transcriptional activator|Transcriptional activator]]
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*[[Transcriptional activator 3D structures|Transcriptional activator 3D structures]]
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== References ==
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<references/>
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__TOC__
__TOC__
</StructureSection>
</StructureSection>
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[[Category: Pseae]]
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[[Category: Large Structures]]
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[[Category: Dong, S H]]
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[[Category: Pseudomonas aeruginosa PAO1]]
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[[Category: Nair, S K]]
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[[Category: Dong SH]]
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[[Category: Luxr receptor]]
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[[Category: Nair SK]]
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[[Category: Signaling protein]]
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[[Category: Signaling protein-agonist complex]]
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Current revision

The structure of ligand binding domain of LasR in complex with TP-1 homolog, compound 13

PDB ID 6d6d

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