4bul
From Proteopedia
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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]] 2.60Å' scene=''> | + | <StructureSection load='4bul' size='340' side='right'caption='[[4bul]], [[Resolution|resolution]] 2.60Å' scene=''> |
== Structural highlights == | == Structural highlights == | ||
| - | <table><tr><td colspan='2'>[[4bul]] is a 6 chain structure with sequence from [ | + | <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]] 2.6Å</td></tr> |
| - | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[ | + | <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 == | ||
| + | [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®/PubMed®, a database of the U.S. National Library of Medicine.<br> | From MEDLINE®/PubMed®, 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: | + | [[Category: Large Structures]] |
| - | [[Category: Bax | + | [[Category: Staphylococcus aureus]] |
| - | [[Category: Brooks | + | [[Category: Synthetic construct]] |
| - | [[Category: Brown | + | [[Category: Bax B]] |
| - | [[Category: Brown | + | [[Category: Brooks G]] |
| - | [[Category: Cailleau | + | [[Category: Brown BS]] |
| - | [[Category: Chen | + | [[Category: Brown P]] |
| - | [[Category: Dabbs | + | [[Category: Cailleau N]] |
| - | [[Category: Davies | + | [[Category: Chen D]] |
| - | [[Category: Esken | + | [[Category: Dabbs S]] |
| - | [[Category: Giordano | + | [[Category: Davies DT]] |
| - | [[Category: Gwynn | + | [[Category: Esken JM]] |
| - | [[Category: Hennessy | + | [[Category: Giordano I]] |
| - | [[Category: Hoover | + | [[Category: Gwynn MN]] |
| - | [[Category: Huang | + | [[Category: Hennessy AJ]] |
| - | [[Category: Jones | + | [[Category: Hoover JL]] |
| - | [[Category: Markwell | + | [[Category: Huang J]] |
| - | [[Category: Miles | + | [[Category: Jones GE]] |
| - | [[Category: Minthorn | + | [[Category: Markwell RE]] |
| - | [[Category: Pearson | + | [[Category: Miles TJ]] |
| - | [[Category: Rittenhouse | + | [[Category: Minthorn EA]] |
| - | [[Category: Spitzfaden | + | [[Category: Pearson ND]] |
| - | [[Category: Sukmar | + | [[Category: Rittenhouse S]] |
| - | + | [[Category: Spitzfaden C]] | |
| - | + | [[Category: Sukmar SKK]] | |
| - | + | ||
Current revision
Novel hydroxyl tricyclics (e.g. GSK966587) as potent inhibitors of bacterial type IIA topoisomerases
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Categories: Large Structures | Staphylococcus aureus | Synthetic construct | Bax B | Brooks G | Brown BS | Brown P | Cailleau N | Chen D | Dabbs S | Davies DT | Esken JM | Giordano I | Gwynn MN | Hennessy AJ | Hoover JL | Huang J | Jones GE | Markwell RE | Miles TJ | Minthorn EA | Pearson ND | Rittenhouse S | Spitzfaden C | Sukmar SKK
