|
|
| Line 1: |
Line 1: |
| | | | |
| | ==Structure of the Staphylococcus aureus AgrA LytTR Domain== | | ==Structure of the Staphylococcus aureus AgrA LytTR Domain== |
| - | <StructureSection load='4g4k' size='340' side='right' caption='[[4g4k]], [[Resolution|resolution]] 1.52Å' scene=''> | + | <StructureSection load='4g4k' size='340' side='right'caption='[[4g4k]], [[Resolution|resolution]] 1.52Å' scene=''> |
| | == Structural highlights == | | == Structural highlights == |
| - | <table><tr><td colspan='2'>[[4g4k]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/"micrococcus_aureus"_(rosenbach_1884)_zopf_1885 "micrococcus aureus" (rosenbach 1884) zopf 1885]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4G4K OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4G4K FirstGlance]. <br> | + | <table><tr><td colspan='2'>[[4g4k]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Staphylococcus_aureus Staphylococcus aureus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4G4K OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4G4K FirstGlance]. <br> |
| - | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=GOL:GLYCEROL'>GOL</scene></td></tr> | + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=GOL:GLYCEROL'>GOL</scene></td></tr> |
| - | <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[3bs1|3bs1]]</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=4g4k FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4g4k OCA], [https://pdbe.org/4g4k PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4g4k RCSB], [https://www.ebi.ac.uk/pdbsum/4g4k PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4g4k ProSAT]</span></td></tr> |
| - | <tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">agr, agrA ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=1280 "Micrococcus aureus" (Rosenbach 1884) Zopf 1885])</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=4g4k FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4g4k OCA], [http://pdbe.org/4g4k PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4g4k RCSB], [http://www.ebi.ac.uk/pdbsum/4g4k PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=4g4k ProSAT]</span></td></tr> | + | |
| | </table> | | </table> |
| | == Function == | | == Function == |
| - | [[http://www.uniprot.org/uniprot/AGRA_STAAU AGRA_STAAU]] Required for high-level post-exponential phase expression of a series of secreted proteins. | + | [https://www.uniprot.org/uniprot/AGRA_STAAU AGRA_STAAU] Required for high-level post-exponential phase expression of a series of secreted proteins. |
| | <div style="background-color:#fffaf0;"> | | <div style="background-color:#fffaf0;"> |
| | == Publication Abstract from PubMed == | | == Publication Abstract from PubMed == |
| Line 24: |
Line 22: |
| | __TOC__ | | __TOC__ |
| | </StructureSection> | | </StructureSection> |
| - | [[Category: Bezar, I F]] | + | [[Category: Large Structures]] |
| - | [[Category: Leonard, P G]] | + | [[Category: Staphylococcus aureus]] |
| - | [[Category: Stock, A M]] | + | [[Category: Bezar IF]] |
| - | [[Category: Activator]] | + | [[Category: Leonard PG]] |
| - | [[Category: Agra]] | + | [[Category: Stock AM]] |
| - | [[Category: Dna binding protein]]
| + | |
| - | [[Category: Lyttr domain]]
| + | |
| - | [[Category: Phosphoprotein]]
| + | |
| - | [[Category: Response regulator]]
| + | |
| - | [[Category: Transcription factor]]
| + | |
| - | [[Category: Transcription regulation]]
| + | |
| - | [[Category: Two-component system]]
| + | |
| Structural highlights
Function
AGRA_STAAU Required for high-level post-exponential phase expression of a series of secreted proteins.
Publication Abstract from PubMed
The AgrA transcription factor regulates the quorum-sensing response in Staphylococcus aureus, controlling the production of hemolysins and other virulence factors. AgrA binds to DNA via its C-terminal LytTR domain, a domain not found in humans but common in many pathogenic bacteria, making it a potential target for antimicrobial development. We have determined the crystal structure of the apo AgrA LytTR domain and screened a library of 500 fragment compounds to find inhibitors of AgrA DNA binding activity. Using nuclear magnetic resonance, the binding site for five compounds has been mapped to a common locus at the C-terminal end of the LytTR domain, a site known to be important for DNA binding activity. Three of these compounds inhibit AgrA DNA binding. These results provide the first evidence that LytTR domains can be targeted by small organic compounds.
Identification of a Hydrophobic Cleft in the LytTR Domain of AgrA as a Locus for Small Molecule Interactions That Inhibit DNA Binding.,Leonard PG, Bezar IF, Sidote DJ, Stock AM Biochemistry. 2012 Dec 18;51(50):10035-43. doi: 10.1021/bi3011785. Epub 2012 Dec , 3. PMID:23181972[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
References
- ↑ Leonard PG, Bezar IF, Sidote DJ, Stock AM. Identification of a Hydrophobic Cleft in the LytTR Domain of AgrA as a Locus for Small Molecule Interactions That Inhibit DNA Binding. Biochemistry. 2012 Dec 18;51(50):10035-43. doi: 10.1021/bi3011785. Epub 2012 Dec , 3. PMID:23181972 doi:http://dx.doi.org/10.1021/bi3011785
|
