3lpg

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{{Seed}}
 
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[[Image:3lpg.jpg|left|200px]]
 
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==Structure of E. coli beta-Glucuronidase bound with a novel, potent inhibitor 3-(2-fluorophenyl)-1-(2-hydroxyethyl)-1-((6-methyl-2-oxo-1,2-dihydroquinolin-3-yl)methyl)urea==
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The line below this paragraph, containing "STRUCTURE_3lpg", creates the "Structure Box" on the page.
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<StructureSection load='3lpg' size='340' side='right'caption='[[3lpg]], [[Resolution|resolution]] 2.42&Aring;' scene=''>
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== Structural highlights ==
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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<table><tr><td colspan='2'>[[3lpg]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Escherichia_coli_K-12 Escherichia coli K-12]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3LPG OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3LPG FirstGlance]. <br>
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</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.425&#8491;</td></tr>
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=MSE:SELENOMETHIONINE'>MSE</scene>, <scene name='pdbligand=Z78:3-(2-FLUOROPHENYL)-1-(2-HYDROXYETHYL)-1-[(6-METHYL-2-OXO-1,2-DIHYDROQUINOLIN-3-YL)METHYL]UREA'>Z78</scene></td></tr>
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{{STRUCTURE_3lpg| PDB=3lpg | SCENE= }}
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=3lpg FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3lpg OCA], [https://pdbe.org/3lpg PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3lpg RCSB], [https://www.ebi.ac.uk/pdbsum/3lpg PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3lpg ProSAT]</span></td></tr>
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</table>
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== Function ==
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[https://www.uniprot.org/uniprot/BGLR_ECOLI BGLR_ECOLI]
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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The dose-limiting side effect of the common colon cancer chemotherapeutic CPT-11 is severe diarrhea caused by symbiotic bacterial beta-glucuronidases that reactivate the drug in the gut. We sought to target these enzymes without killing the commensal bacteria essential for human health. Potent bacterial beta-glucuronidase inhibitors were identified by high-throughput screening and shown to have no effect on the orthologous mammalian enzyme. Crystal structures established that selectivity was based on a loop unique to bacterial beta-glucuronidases. Inhibitors were highly effective against the enzyme target in living aerobic and anaerobic bacteria, but did not kill the bacteria or harm mammalian cells. Finally, oral administration of an inhibitor protected mice from CPT-11-induced toxicity. Thus, drugs may be designed to inhibit undesirable enzyme activities in essential microbial symbiotes to enhance chemotherapeutic efficacy.
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===Structure of E. coli beta-Glucuronidase bound with a novel, potent inhibitor 3-(2-fluorophenyl)-1-(2-hydroxyethyl)-1-((6-methyl-2-oxo-1,2-dihydroquinolin-3-yl)methyl)urea===
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Alleviating cancer drug toxicity by inhibiting a bacterial enzyme.,Wallace BD, Wang H, Lane KT, Scott JE, Orans J, Koo JS, Venkatesh M, Jobin C, Yeh LA, Mani S, Redinbo MR Science. 2010 Nov 5;330(6005):831-5. PMID:21051639<ref>PMID:21051639</ref>
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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</div>
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<div class="pdbe-citations 3lpg" style="background-color:#fffaf0;"></div>
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==See Also==
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*[[Glucuronisidase 3D structures|Glucuronisidase 3D structures]]
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(as it appears on PubMed at http://www.pubmed.gov), where 21051639 is the PubMed ID number.
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== References ==
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<references/>
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{{ABSTRACT_PUBMED_21051639}}
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__TOC__
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</StructureSection>
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==About this Structure==
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[[Category: Escherichia coli K-12]]
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3LPG is a 2 chains structure with sequences from [http://en.wikipedia.org/wiki/Escherichia_coli Escherichia coli]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3LPG OCA].
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[[Category: Large Structures]]
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[[Category: Redinbo MR]]
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==Reference==
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[[Category: Wallace BD]]
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<ref group="xtra">PMID:21051639</ref><references group="xtra"/>
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[[Category: Beta-glucuronidase]]
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[[Category: Escherichia coli]]
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[[Category: Redinbo, M R.]]
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[[Category: Wallace, B D.]]
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[[Category: Alpha/beta barrel]]
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[[Category: Beta-sandwich domain]]
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[[Category: Glycosidase]]
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[[Category: Glycosyl hydrolase]]
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[[Category: Hydrolase]]
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[[Category: Hydrolase-hydrolase inhibitor complex]]
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[[Category: Sugar-binding domain]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Nov 18 00:49:41 2010''
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Current revision

Structure of E. coli beta-Glucuronidase bound with a novel, potent inhibitor 3-(2-fluorophenyl)-1-(2-hydroxyethyl)-1-((6-methyl-2-oxo-1,2-dihydroquinolin-3-yl)methyl)urea

PDB ID 3lpg

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