5xe8
From Proteopedia
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| - | '''Unreleased structure''' | ||
| - | + | ==Crystal Structure of the Peptidase Domain of Streptococcus mutans ComA== | |
| + | <StructureSection load='5xe8' size='340' side='right' caption='[[5xe8]], [[Resolution|resolution]] 3.10Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[5xe8]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5XE8 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5XE8 FirstGlance]. <br> | ||
| + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=PEG:DI(HYDROXYETHYL)ETHER'>PEG</scene></td></tr> | ||
| + | <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[5xe9|5xe9]]</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=5xe8 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5xe8 OCA], [http://pdbe.org/5xe8 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5xe8 RCSB], [http://www.ebi.ac.uk/pdbsum/5xe8 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5xe8 ProSAT]</span></td></tr> | ||
| + | </table> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | The main components of the quorum-sensing system are expected to be favorable targets for drug development to combat various chronic infectious diseases. ComA of Streptococcus is an ATP-binding cassette transporter containing a peptidase domain (PEP), which is essential for the quorum-sensing signal production. Using high-throughput screening, we found a potent small molecule that suppressed the S. mutans quorum-sensing pathway through inhibition of PEP activity. The compound effectively attenuated the biofilm formation and competence development of S. mutans without inhibiting cell growth. The kinetic and structural studies with this molecule and a related compound unexpectedly revealed an allosteric site of PEP. This relatively hydrophobic site is thought to undergo large structural changes during the catalytic process. These compounds inhibit PEP activity by binding to and suppressing the structural changes of this site. These results showed that PEP is a good target for inhibitors of the Streptococcus quorum-sensing system. | ||
| - | + | High-throughput Screening of Small Molecule Inhibitors of the Streptococcus Quorum-sensing Signal Pathway.,Ishii S, Fukui K, Yokoshima S, Kumagai K, Beniyama Y, Kodama T, Fukuyama T, Okabe T, Nagano T, Kojima H, Yano T Sci Rep. 2017 Jun 22;7(1):4029. doi: 10.1038/s41598-017-03567-2. PMID:28642545<ref>PMID:28642545</ref> | |
| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| - | [[Category: | + | </div> |
| + | <div class="pdbe-citations 5xe8" style="background-color:#fffaf0;"></div> | ||
| + | == References == | ||
| + | <references/> | ||
| + | __TOC__ | ||
| + | </StructureSection> | ||
| + | [[Category: Beniyama, Y]] | ||
| + | [[Category: Fukui, K]] | ||
| + | [[Category: Fukuyama, T]] | ||
| + | [[Category: Ishii, S]] | ||
| + | [[Category: Kodama, T]] | ||
| + | [[Category: Kojima, H]] | ||
| + | [[Category: Kumagai, K]] | ||
| + | [[Category: Nagano, T]] | ||
| + | [[Category: Okabe, T]] | ||
| + | [[Category: Yano, T]] | ||
| + | [[Category: Yokoshima, S]] | ||
| + | [[Category: Hydrolase-hydrolase inhibitor complex]] | ||
| + | [[Category: Peptidase]] | ||
| + | [[Category: Quorum-sensing]] | ||
Revision as of 06:02, 17 August 2017
Crystal Structure of the Peptidase Domain of Streptococcus mutans ComA
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