View source for 5znx


==Crystal structure of CM14-treated HlyU from Vibrio vulnificus==
<StructureSection load='5znx' size='340' side='right'caption='[[5znx]], [[Resolution|resolution]] 2.11&Aring;' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>[[5znx]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Vibrio_vulnificus_CMCP6 Vibrio vulnificus CMCP6]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5ZNX OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5ZNX FirstGlance]. <br>
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.114&#8491;</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=5znx FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5znx OCA], [https://pdbe.org/5znx PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5znx RCSB], [https://www.ebi.ac.uk/pdbsum/5znx PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5znx ProSAT]</span></td></tr>
</table>
== Function ==
[https://www.uniprot.org/uniprot/A0A3Q0L222_VIBVU A0A3Q0L222_VIBVU] 
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
Increasing antibiotic resistance has led to the development of new strategies to combat bacterial infection. Anti-virulence strategies that impair virulence of bacterial pathogens are one of the novel approaches with less selective pressure for developing resistance than traditional strategies that impede viability. In this study, a small molecule CM14 [N-(4-oxo-4H-thieno[3,4-c]chromen-3-yl)-3-phenylprop-2-ynamide] that inhibits the activity of HlyU, a transcriptional regulator essential for the virulence of the fulminating human pathogen Vibrio vulnificus, has been identified. Without affecting bacterial growth or triggering the host cell death, CM14 reduces HlyU-dependent expression of virulence genes in V. vulnificus. In addition to the decreased hemolysis of human erythrocytes, CM14 impedes host cell rounding and lysis caused by V. vulnificus. Notably, CM14 significantly enhances survival of mice infected with V. vulnificus by alleviating hepatic and renal dysfunction and systemic inflammation. Biochemical, mass spectrometric, and mutational analyses revealed that CM14 inhibits HlyU from binding to target DNA by covalently modifying Cys30. Remarkably, CM14 decreases the expression of various virulence genes of other Vibrio species and thus attenuates their virulence phenotypes. Together, this molecule could be an anti-virulence agent against HlyU-harboring Vibrio species with a low selective pressure for the emergence of resistance.

Small-molecule inhibitor of HlyU attenuates virulence of Vibrio species.,Lee ZW, Kim BS, Jang KK, Bang YJ, Kim S, Ha NC, Jung YH, Lee HJ, Han HJ, Kim JS, Kim J, Sahu PK, Jeong LS, Kim MH, Choi SH Sci Rep. 2019 Mar 13;9(1):4346. doi: 10.1038/s41598-019-39554-y. PMID:30867441<ref>PMID:30867441</ref>

From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
</div>
<div class="pdbe-citations 5znx" style="background-color:#fffaf0;"></div>

==See Also==
*[[Transcriptional activator 3D structures|Transcriptional activator 3D structures]]
== References ==
<references/>
__TOC__
</StructureSection>
[[Category: Large Structures]]
[[Category: Vibrio vulnificus CMCP6]]
[[Category: Ahn J]]
[[Category: Baek Y]]
[[Category: Hong S]]
[[Category: Jeong S]]
[[Category: Jo I]]
[[Category: Kim S]]
[[Category: Park N]]