6d6p: Difference between revisions
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<StructureSection load='6d6p' size='340' side='right' caption='[[6d6p]], [[Resolution|resolution]] 1.65Å' scene=''> | <StructureSection load='6d6p' size='340' side='right' caption='[[6d6p]], [[Resolution|resolution]] 1.65Å' scene=''> | ||
== Structural highlights == | == Structural highlights == | ||
<table><tr><td colspan='2'>[[6d6p]] is a 4 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6D6P OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6D6P FirstGlance]. <br> | <table><tr><td colspan='2'>[[6d6p]] is a 4 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=6D6P OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6D6P FirstGlance]. <br> | ||
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=FY1:N-{[3,5-dibromo-2-(methoxymethoxy)phenyl]methyl}-2-nitrobenzamide'>FY1</scene></td></tr> | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=FY1:N-{[3,5-dibromo-2-(methoxymethoxy)phenyl]methyl}-2-nitrobenzamide'>FY1</scene></td></tr> | ||
<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[6d6a|6d6a]], [[6d6b|6d6b]], [[6d6c|6d6c]], [[6d6d|6d6d]], [[6d6l|6d6l]], [[6d6m|6d6m]], [[6d6n|6d6n]], [[6d6o|6d6o]]</td></tr> | <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[6d6a|6d6a]], [[6d6b|6d6b]], [[6d6c|6d6c]], [[6d6d|6d6d]], [[6d6l|6d6l]], [[6d6m|6d6m]], [[6d6n|6d6n]], [[6d6o|6d6o]]</td></tr> | ||
<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> | |||
<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=6d6p FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6d6p OCA], [http://pdbe.org/6d6p PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6d6p RCSB], [http://www.ebi.ac.uk/pdbsum/6d6p PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6d6p 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=6d6p FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6d6p OCA], [http://pdbe.org/6d6p PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6d6p RCSB], [http://www.ebi.ac.uk/pdbsum/6d6p PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6d6p ProSAT]</span></td></tr> | ||
</table> | </table> | ||
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</div> | </div> | ||
<div class="pdbe-citations 6d6p" style="background-color:#fffaf0;"></div> | <div class="pdbe-citations 6d6p" style="background-color:#fffaf0;"></div> | ||
==See Also== | |||
*[[Transcriptional activator|Transcriptional activator]] | |||
== References == | == References == | ||
<references/> | <references/> | ||
__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
[[Category: Pseae]] | |||
[[Category: Dong, S H]] | [[Category: Dong, S H]] | ||
[[Category: Nair, S K]] | [[Category: Nair, S K]] | ||
[[Category: Luxr receptor]] | [[Category: Luxr receptor]] | ||
[[Category: Signaling protein-agonist complex]] | [[Category: Signaling protein-agonist complex]] | ||
Revision as of 11:46, 3 October 2018
The structure of ligand binding domain of LasR in complex with TP-1 homolog, compound 19The structure of ligand binding domain of LasR in complex with TP-1 homolog, compound 19
Structural highlights
Function[LASR_PSEAE] Transcriptional activator of elastase structural gene (LasB). Binds to the PAI autoinducer. Publication Abstract from PubMedChemical 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. 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[1] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See AlsoReferences
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