4xyc

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'''Unreleased structure'''
 
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The entry 4xyc is ON HOLD until Paper Publication
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==NANOMOLAR INHIBITORS OF MYCOBACTERIUM TUBERCULOSIS GLUTAMINE SYNTHETASE 1: SYNTHESIS, BIOLOGICAL EVALUATION AND X-RAY CRYSTALLOGRAPHIC STUDIES==
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<StructureSection load='4xyc' size='340' side='right'caption='[[4xyc]], [[Resolution|resolution]] 3.30&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[4xyc]] is a 24 chain structure with sequence from [https://en.wikipedia.org/wiki/Mycobacterium_tuberculosis Mycobacterium tuberculosis]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4XYC OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4XYC 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]] 3.3&#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=2K9:9-PHENYL-4H-IMIDAZO[1,2-A]INDENO[1,2-E]PYRAZIN-4-ONE'>2K9</scene></td></tr>
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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=4xyc FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4xyc OCA], [https://pdbe.org/4xyc PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4xyc RCSB], [https://www.ebi.ac.uk/pdbsum/4xyc PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4xyc ProSAT]</span></td></tr>
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</table>
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== Function ==
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[https://www.uniprot.org/uniprot/GLN1B_MYCTO GLN1B_MYCTO] Involved in nitrogen metabolism via ammonium assimilation. Catalyzes the ATP-dependent biosynthesis of glutamine from glutamate and ammonia. Also plays a key role in controlling the ammonia levels within infected host cells and so contributes to the pathogens capacity to inhibit phagosome acidification and phagosome-lysosome fusion. Involved in cell wall biosynthesis via the production of the major component poly-L-glutamine (PLG). PLG synthesis in the cell wall occurs only in nitrogen limiting conditions and on the contrary high nitrogen conditions inhibit PLG synthesis.[UniProtKB:P9WN39]
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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A series of imidazo[1,2-a]indeno[1,2-e]pyrazin-4-ones that potently inhibit M. tuberculosis glutamine synthetase (GlnA1) has been identified by high throughput screening. Exploration of this series was performed owing to a short chemistry program. Despite possibly nanomolar inhibitions, none of these compounds was active on whole cell Mtb, suggesting that GlnA1 may not be a suitable target to find new anti-tubercular drugs.
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Authors: Couturier, C., Silve, S., Morales, R., Ppessegue, B., Llopart, S., Nair, A., Bauer, A., Scheiper, B., poeverlein, c., Ganzhorn, A., Lagrange, S., Bacque, E.
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Nanomolar inhibitors of Mycobacterium tuberculosis glutamine synthetase 1: Synthesis, biological evaluation and X-ray crystallographic studies.,Couturier C, Silve S, Morales R, Pessegue B, Llopart S, Nair A, Bauer A, Scheiper B, Poverlein C, Ganzhorn A, Lagrange S, Bacque E Bioorg Med Chem Lett. 2015 Apr 1;25(7):1455-9. doi: 10.1016/j.bmcl.2015.02.035., Epub 2015 Feb 23. PMID:25770781<ref>PMID:25770781</ref>
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Description: NANOMOLAR INHIBITORS OF MYCOBACTERIUM TUBERCULOSIS GLUTAMINE SYNTHETASE 1: SYNTHESIS, BIOLOGICAL EVALUATION AND X-RAY CRYSTALLOGRAPHIC STUDIES
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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[[Category: Unreleased Structures]]
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</div>
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[[Category: Poeverlein, C]]
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<div class="pdbe-citations 4xyc" style="background-color:#fffaf0;"></div>
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[[Category: Llopart, S]]
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[[Category: Ppessegue, B]]
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==See Also==
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[[Category: Morales, R]]
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*[[Glutamine synthetase 3D structures|Glutamine synthetase 3D structures]]
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[[Category: Nair, A]]
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== References ==
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[[Category: Silve, S]]
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<references/>
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[[Category: Lagrange, S]]
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__TOC__
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[[Category: Bacque, E]]
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</StructureSection>
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[[Category: Bauer, A]]
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[[Category: Large Structures]]
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[[Category: Ganzhorn, A]]
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[[Category: Mycobacterium tuberculosis]]
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[[Category: Scheiper, B]]
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[[Category: Bacque E]]
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[[Category: Couturier, C]]
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[[Category: Bauer A]]
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[[Category: Couturier C]]
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[[Category: Ganzhorn A]]
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[[Category: Lagrange S]]
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[[Category: Llopart S]]
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[[Category: Morales R]]
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[[Category: Nair A]]
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[[Category: Ppessegue B]]
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[[Category: Scheiper B]]
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[[Category: Silve S]]
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[[Category: Poeverlein c]]

Current revision

NANOMOLAR INHIBITORS OF MYCOBACTERIUM TUBERCULOSIS GLUTAMINE SYNTHETASE 1: SYNTHESIS, BIOLOGICAL EVALUATION AND X-RAY CRYSTALLOGRAPHIC STUDIES

PDB ID 4xyc

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