4xyc
From Proteopedia
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| - | ''' | + | ==NANOMOLAR INHIBITORS OF MYCOBACTERIUM TUBERCULOSIS GLUTAMINE SYNTHETASE 1: SYNTHESIS, BIOLOGICAL EVALUATION AND X-RAY CRYSTALLOGRAPHIC STUDIES== |
| + | <StructureSection load='4xyc' size='340' side='right' caption='[[4xyc]], [[Resolution|resolution]] 3.30Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[4xyc]] is a 24 chain structure. 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 [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4XYC FirstGlance]. <br> | ||
| + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=2K9:9-PHENYL-4H-IMIDAZO[1,2-A]INDENO[1,2-E]PYRAZIN-4-ONE'>2K9</scene></td></tr> | ||
| + | <tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Glutamate--ammonia_ligase Glutamate--ammonia ligase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=6.3.1.2 6.3.1.2] </span></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=4xyc FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4xyc OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4xyc RCSB], [http://www.ebi.ac.uk/pdbsum/4xyc PDBsum]</span></td></tr> | ||
| + | </table> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | 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. | ||
| - | + | 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> | |
| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| - | + | </div> | |
| - | + | == References == | |
| - | [[Category: | + | <references/> |
| - | [[Category: | + | __TOC__ |
| + | </StructureSection> | ||
| + | [[Category: Glutamate--ammonia ligase]] | ||
| + | [[Category: Bacque, E]] | ||
| + | [[Category: Bauer, A]] | ||
| + | [[Category: Couturier, C]] | ||
| + | [[Category: Ganzhorn, A]] | ||
| + | [[Category: Lagrange, S]] | ||
[[Category: Llopart, S]] | [[Category: Llopart, S]] | ||
| - | [[Category: Ppessegue, B]] | ||
[[Category: Morales, R]] | [[Category: Morales, R]] | ||
[[Category: Nair, A]] | [[Category: Nair, A]] | ||
| + | [[Category: Ppessegue, B]] | ||
| + | [[Category: Scheiper, B]] | ||
[[Category: Silve, S]] | [[Category: Silve, S]] | ||
| - | [[Category: | + | [[Category: Poeverlein, c]] |
| - | [[Category: | + | [[Category: Atp binding]] |
| - | [[Category: | + | [[Category: Ligase]] |
| - | [[Category: | + | [[Category: Ligase-ligase inhibitor complex]] |
| - | + | ||
| - | + | ||
Revision as of 14:02, 26 March 2015
NANOMOLAR INHIBITORS OF MYCOBACTERIUM TUBERCULOSIS GLUTAMINE SYNTHETASE 1: SYNTHESIS, BIOLOGICAL EVALUATION AND X-RAY CRYSTALLOGRAPHIC STUDIES
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