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==Novel hydroxyl tricyclics (e.g. GSK966587) as potent inhibitors of bacterial type IIA topoisomerases==
==Novel hydroxyl tricyclics (e.g. GSK966587) as potent inhibitors of bacterial type IIA topoisomerases==
<StructureSection load='4bul' size='340' side='right' caption='[[4bul]], [[Resolution|resolution]] 2.60&Aring;' scene=''>
<StructureSection load='4bul' size='340' side='right'caption='[[4bul]], [[Resolution|resolution]] 2.60&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
<table><tr><td colspan='2'>[[4bul]] is a 6 chain structure with sequence from [http://en.wikipedia.org/wiki/Staan Staan]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4BUL OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4BUL FirstGlance]. <br>
<table><tr><td colspan='2'>[[4bul]] is a 6 chain structure with sequence from [https://en.wikipedia.org/wiki/Staphylococcus_aureus Staphylococcus aureus] and [https://en.wikipedia.org/wiki/Synthetic_construct Synthetic construct]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4BUL OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4BUL FirstGlance]. <br>
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=AE8:(S)-4-((4-(((2,3-DIHYDRO-[1,4]DIOXINO[2,3-C]PYRIDIN-7-YL)METHYL)AMINO)PIPERIDIN-1-YL)METHYL)-3-FLUORO-4-HYDROXY-4H-PYRROLO[3,2,1-DE][1,5]NAPHTHYRIDIN-7(5H)-ONE'>AE8</scene>, <scene name='pdbligand=MN:MANGANESE+(II)+ION'>MN</scene></td></tr>
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.6&#8491;</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=4bul FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4bul OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4bul RCSB], [http://www.ebi.ac.uk/pdbsum/4bul PDBsum]</span></td></tr>
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=AE8:(S)-4-((4-(((2,3-DIHYDRO-[1,4]DIOXINO[2,3-C]PYRIDIN-7-YL)METHYL)AMINO)PIPERIDIN-1-YL)METHYL)-3-FLUORO-4-HYDROXY-4H-PYRROLO[3,2,1-DE][1,5]NAPHTHYRIDIN-7(5H)-ONE'>AE8</scene>, <scene name='pdbligand=MN:MANGANESE+(II)+ION'>MN</scene></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=4bul FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4bul OCA], [https://pdbe.org/4bul PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4bul RCSB], [https://www.ebi.ac.uk/pdbsum/4bul PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4bul ProSAT]</span></td></tr>
</table>
</table>
== Function ==
== Function ==
[[http://www.uniprot.org/uniprot/GYRB_STAAN GYRB_STAAN]] DNA gyrase negatively supercoils closed circular double-stranded DNA in an ATP-dependent manner and also catalyzes the interconversion of other topological isomers of double-stranded DNA rings, including catenanes and knotted rings (By similarity).  
[https://www.uniprot.org/uniprot/GYRA_STAAN GYRA_STAAN] DNA gyrase negatively supercoils closed circular double-stranded DNA in an ATP-dependent manner and also catalyzes the interconversion of other topological isomers of double-stranded DNA rings, including catenanes and knotted rings.[HAMAP-Rule:MF_01897][https://www.uniprot.org/uniprot/GYRB_STAAN GYRB_STAAN] DNA gyrase negatively supercoils closed circular double-stranded DNA in an ATP-dependent manner and also catalyzes the interconversion of other topological isomers of double-stranded DNA rings, including catenanes and knotted rings (By similarity).
<div style="background-color:#fffaf0;">
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
== Publication Abstract from PubMed ==
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
</div>
</div>
<div class="pdbe-citations 4bul" style="background-color:#fffaf0;"></div>


==See Also==
==See Also==
*[[Gyrase|Gyrase]]
*[[Gyrase 3D Structures|Gyrase 3D Structures]]
== References ==
== References ==
<references/>
<references/>
__TOC__
__TOC__
</StructureSection>
</StructureSection>
[[Category: Staan]]
[[Category: Large Structures]]
[[Category: Bax, B]]
[[Category: Staphylococcus aureus]]
[[Category: Brooks, G]]
[[Category: Synthetic construct]]
[[Category: Brown, B S]]
[[Category: Bax B]]
[[Category: Brown, P]]
[[Category: Brooks G]]
[[Category: Cailleau, N]]
[[Category: Brown BS]]
[[Category: Chen, D]]
[[Category: Brown P]]
[[Category: Dabbs, S]]
[[Category: Cailleau N]]
[[Category: Davies, D T]]
[[Category: Chen D]]
[[Category: Esken, J M]]
[[Category: Dabbs S]]
[[Category: Giordano, I]]
[[Category: Davies DT]]
[[Category: Gwynn, M N]]
[[Category: Esken JM]]
[[Category: Hennessy, A J]]
[[Category: Giordano I]]
[[Category: Hoover, J L]]
[[Category: Gwynn MN]]
[[Category: Huang, J]]
[[Category: Hennessy AJ]]
[[Category: Jones, G E]]
[[Category: Hoover JL]]
[[Category: Markwell, R E]]
[[Category: Huang J]]
[[Category: Miles, T J]]
[[Category: Jones GE]]
[[Category: Minthorn, E A]]
[[Category: Markwell RE]]
[[Category: Pearson, N D]]
[[Category: Miles TJ]]
[[Category: Rittenhouse, S]]
[[Category: Minthorn EA]]
[[Category: Spitzfaden, C]]
[[Category: Pearson ND]]
[[Category: Sukmar, S K.K]]
[[Category: Rittenhouse S]]
[[Category: Isomerase]]
[[Category: Spitzfaden C]]
[[Category: Nbti]]
[[Category: Sukmar SKK]]
[[Category: Type iia topoisomerase]]