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| - | ==Crystal structure of the E. coli ribosome bound to dalfopristin and quinupristin. This file contains the 50S subunit of the second 70S ribosome with dalfopristin and quinupristin bound.==
| + | #REDIRECT [[4u26]] This PDB entry is obsolete and replaced by 4u26 |
| - | <StructureSection load='4tpb' size='340' side='right' caption='[[4tpb]], [[Resolution|resolution]] 2.80Å' scene=''>
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| - | == Structural highlights ==
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| - | <table><tr><td colspan='2'>[[4tpb]] is a 31 chain structure with sequence from [http://en.wikipedia.org/wiki/Escherichia_coli Escherichia coli] and [http://en.wikipedia.org/wiki/Escherichia_coli_str._k-12_substr._mds42 Escherichia coli str. k-12 substr. mds42]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4TPB OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4TPB FirstGlance]. <br>
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| - | </td></tr><tr><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=DOL:5-(2-DIETHYLAMINO-ETHANESULFONYL)-21-HYDROXY-10-ISOPROPYL-11,19-DIMETHYL-9,26-DIOXA-3,15,28-TRIAZA-TRICYCLO[23.2.1.00,255]OCTACOSA-1(27),12,17,19,25(28)-PENTAENE-2,8,14,23-TETRAONE'>DOL</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene><br>
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| - | <tr><td class="sblockLbl"><b>[[Non-Standard_Residue|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=004:(2S)-AMINO(PHENYL)ETHANOIC+ACID'>004</scene>, <scene name='pdbligand=DBB:D-ALPHA-AMINOBUTYRIC+ACID'>DBB</scene>, <scene name='pdbligand=MHT:(3S)-3-(METHYLSULFANYL)-1-AZABICYCLO[2.2.2]OCTANE'>MHT</scene>, <scene name='pdbligand=MHU:4-N,N-(DIMETHYLAMINO)-L-PHENYLALANINE'>MHU</scene>, <scene name='pdbligand=MHV:4-OXO-L-PIPECOLIC+ACID'>MHV</scene>, <scene name='pdbligand=MHW:3-HYDROXYPICOLINIC+ACID'>MHW</scene></td></tr>
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| - | <tr><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[4tp8|4tp8]], [[4tp9|4tp9]], [[4tpa|4tpa]]</td></tr>
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| - | <tr><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4tpb FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4tpb OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4tpb RCSB], [http://www.ebi.ac.uk/pdbsum/4tpb PDBsum]</span></td></tr>
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| - | <table>
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| - | <div style="background-color:#fffaf0;">
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| - | == Publication Abstract from PubMed ==
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| - | Streptogramin antibiotics are divided into type A and B streptogramins, which in combination can act synergistically. We compared the molecular interactions of the streptogramin combinations Synercid (type A: dalfopristin, type B: quinupristin) and NXL 103 (type A: flopristin, type B: linopristin) with the Escherichia coli 70S ribosome by x-ray crystallography. We further analyzed the activity of the streptogramin components individually and in combination. Streptogramin A and B components in Synercid and NXL 103 exhibit synergistic antimicrobial activity against certain pathogenic bacteria. However, in transcription-coupled translation assays, only combinations that include dalfopristin, the streptogramin A component of Synercid, show synergy. Notably, the diethylaminoethylsulfonyl group in dalfopristin reduces its activity, but is the basis for synergy in transcription-coupled translation assays before its rapid hydrolysis from the depsipeptide core. Replacement of the diethylaminoethylsulfonyl group in dalfopristin by a non-hydrolyzable group may therefore be beneficial for synergy. The absence of general streptogramin synergy in transcription-coupled translation assays suggests that synergistic antimicrobial activity of streptogramins can occur independently of streptogramin effects on translation.
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| - | Synergy of streptogramin antibiotics occurs independently of their effects on translation.,Noeske J, Huang J, Olivier NB, Giacobbe RA, Zambrowski M, Cate JH Antimicrob Agents Chemother. 2014 Jun 23. pii: AAC.03389-14. PMID:24957822<ref>PMID:24957822</ref>
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| - | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
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| - | </div>
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| - | == References ==
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| - | <references/>
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| - | __TOC__
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| - | </StructureSection>
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| - | [[Category: Escherichia coli]]
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| - | [[Category: Escherichia coli str. k-12 substr. mds42]]
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| - | [[Category: Cate, J H.D.]]
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| - | [[Category: Giacobbe, R A.]]
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| - | [[Category: Huang, J.]]
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| - | [[Category: Noeske, J.]]
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| - | [[Category: Olivier, N B.]]
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| - | [[Category: Zambrowski, M.]]
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| - | [[Category: 23]]
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| - | [[Category: 50]]
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| - | [[Category: 70]]
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| - | [[Category: Antibiotic]]
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| - | [[Category: Exit]]
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| - | [[Category: Peptidyl]]
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| - | [[Category: Protein biosynthesis]]
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| - | [[Category: Ribosomal subunit]]
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| - | [[Category: Ribosome]]
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| - | [[Category: Rna]]
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| - | [[Category: Streptogramin]]
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| - | [[Category: Transfer]]
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| - | [[Category: Trna]]
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