2y6r
From Proteopedia
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| - | [[ | + | ==STRUCTURE OF THE TETX MONOOXYGENASE IN COMPLEX WITH THE SUBSTRATE 7-CHLORTETRACYCLINE== |
| + | <StructureSection load='2y6r' size='340' side='right' caption='[[2y6r]], [[Resolution|resolution]] 3.10Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[2y6r]] is a 4 chain structure with sequence from [http://en.wikipedia.org/wiki/Bacteroides_thetaiotaomicron Bacteroides thetaiotaomicron]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2Y6R OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2Y6R FirstGlance]. <br> | ||
| + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=CTC:7-CHLOROTETRACYCLINE'>CTC</scene>, <scene name='pdbligand=FAD:FLAVIN-ADENINE+DINUCLEOTIDE'>FAD</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr> | ||
| + | <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[2xdo|2xdo]], [[2xyo|2xyo]], [[2y6q|2y6q]]</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=2y6r FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2y6r OCA], [http://www.rcsb.org/pdb/explore.do?structureId=2y6r RCSB], [http://www.ebi.ac.uk/pdbsum/2y6r PDBsum]</span></td></tr> | ||
| + | </table> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | The flavin-dependent monooxygenase TetX confers resistance to all clinically relevant tetracyclines, including the recently approved, broad-spectrum antibiotic tigecycline (Tygacil(R)) which is a critical last-ditch defense against multidrug-resistant pathogens. TetX represents the first resistance mechanism against tigecycline, which circumvents both the tet-gene encoded resistances, relying on active efflux of tetracyclines, and ribosomal protection proteins. The alternative enzyme-based mechanism of TetX depends on regioselective hydroxylation of tetracycline antibiotics to 11a-hydroxy-tetracyclines. Here, we report the X-ray crystallographic structure determinations at 2.1A resolution of native TetX from Bacteroides thetaiotaomicron and its complexes with tetracyclines. Our crystal structures explain the extremely versatile substrate diversity of the enzyme and provide a first step towards the rational design of novel tetracycline derivatives to counter TetX-based resistance prior to emerging clinical observations. | ||
| - | + | Structural basis for a new tetracycline resistance mechanism relying on the TetX monooxygenase.,Volkers G, Palm GJ, Weiss MS, Wright GD, Hinrichs W FEBS Lett. 2011 Mar 16. PMID:21402075<ref>PMID:21402075</ref> | |
| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| - | + | </div> | |
| - | + | == References == | |
| - | + | <references/> | |
| - | + | __TOC__ | |
| - | + | </StructureSection> | |
| - | + | ||
| - | == | + | |
| - | < | + | |
[[Category: Bacteroides thetaiotaomicron]] | [[Category: Bacteroides thetaiotaomicron]] | ||
| - | [[Category: Hinrichs, W | + | [[Category: Hinrichs, W]] |
| - | [[Category: Palm, G J | + | [[Category: Palm, G J]] |
| - | [[Category: Volkers, G | + | [[Category: Volkers, G]] |
| - | [[Category: Weiss, M S | + | [[Category: Weiss, M S]] |
| - | [[Category: Wright, G D | + | [[Category: Wright, G D]] |
[[Category: Antibiotic resistance]] | [[Category: Antibiotic resistance]] | ||
[[Category: Flavin]] | [[Category: Flavin]] | ||
Revision as of 08:50, 26 November 2014
STRUCTURE OF THE TETX MONOOXYGENASE IN COMPLEX WITH THE SUBSTRATE 7-CHLORTETRACYCLINE
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