5n7o: Difference between revisions

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'''Unreleased structure'''


The entry 5n7o is ON HOLD
==EthR2 in complex with SMARt-420 compound==
<StructureSection load='5n7o' size='340' side='right' caption='[[5n7o]], [[Resolution|resolution]] 2.30&Aring;' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>[[5n7o]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5N7O OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5N7O FirstGlance]. <br>
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=69Y:4,4,4-TRIFLUORO-1-(3-PHENYL-1-OXA-2,8-DIAZASPIRO[4.5]DEC-2-EN-8-YL)BUTAN-1-ONE'>69Y</scene></td></tr>
<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[5icj|5icj]], [[5n1c|5n1c]], [[5n1i|5n1i]]</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=5n7o FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5n7o OCA], [http://pdbe.org/5n7o PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5n7o RCSB], [http://www.ebi.ac.uk/pdbsum/5n7o PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5n7o ProSAT]</span></td></tr>
</table>
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
Inhibition of transcriptional regulators of bacterial pathogens with the aim of reprogramming their metabolism to modify their antibiotic susceptibility constitutes a promising therapeutic strategy. One example is the bio-activation of the anti-tubercular pro-drug ethionamide, which activity could be enhanced by inhibiting the transcriptional repressor EthR. Recently, we discovered that inhibition of a second transcriptional repressor, EthR2, leads to the awakening of a new ethionamide bio-activation pathway. The x-ray structure of EthR2 was solved at 2.3 A resolution in complex with a compound called SMARt-420 (Small Molecule Aborting Resistance). Detailed comparison and structural analysis revealed interesting insights for the upcoming structure-based design of EthR2 inhibitors as an alternative to revert ethionamide resistance in Mycobacterium tuberculosis.


Authors: Wohlkonig, A., Wintjens, R.
Structural analysis of the interaction between spiroisoxazoline SMARt-420 and the Mycobacterium tuberculosis repressor EthR2.,Wohlkonig A, Remaut H, Moune M, Tanina A, Meyer F, Desroses M, Steyaert J, Willand N, Baulard AR, Wintjens R Biochem Biophys Res Commun. 2017 Apr 14. pii: S0006-291X(17)30750-7. doi:, 10.1016/j.bbrc.2017.04.074. PMID:28416386<ref>PMID:28416386</ref>


Description: EthR2 in complex with SMARt-420 compound
From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
[[Category: Unreleased Structures]]
</div>
<div class="pdbe-citations 5n7o" style="background-color:#fffaf0;"></div>
== References ==
<references/>
__TOC__
</StructureSection>
[[Category: Wintjens, R]]
[[Category: Wintjens, R]]
[[Category: Wohlkonig, A]]
[[Category: Wohlkonig, A]]
[[Category: Complex]]
[[Category: Inhibitor]]
[[Category: Repressor]]
[[Category: Transcription]]
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