3uo9: Difference between revisions
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[[ | ==Crystal Structure of Human GAC in Complex with Glutamate and BPTES== | ||
<StructureSection load='3uo9' size='340' side='right' caption='[[3uo9]], [[Resolution|resolution]] 2.30Å' scene=''> | |||
== Structural highlights == | |||
<table><tr><td colspan='2'>[[3uo9]] is a 4 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3UO9 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3UO9 FirstGlance]. <br> | |||
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=04A:N,N-[SULFANEDIYLBIS(ETHANE-2,1-DIYL-1,3,4-THIADIAZOLE-5,2-DIYL)]BIS(2-PHENYLACETAMIDE)'>04A</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene></td></tr> | |||
<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[3unw|3unw]]</td></tr> | |||
<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">GLS, GLS1, KIAA0838 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])</td></tr> | |||
<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Glutaminase Glutaminase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.5.1.2 3.5.1.2] </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=3uo9 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3uo9 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3uo9 RCSB], [http://www.ebi.ac.uk/pdbsum/3uo9 PDBsum]</span></td></tr> | |||
</table> | |||
<div style="background-color:#fffaf0;"> | |||
== Publication Abstract from PubMed == | |||
Glutaminase (GLS1/2) catalyzes the conversion of l-glutamine to l-glutamate and ammonia. The level of a splice variant of GLS1 (GAC) is elevated in certain cancers, and GAC is specifically inhibited by bis-2-(5-phenylacetimido-1,2,4,thiadiazol-2-yl)ethyl sulfide (BPTES). We report here the first full-length crystal structure of GAC in the presence and absence of BPTES molecules. Two BPTES molecules bind at an interface region of the GAC tetramer in a manner that appears to lock the GAC tetramer into a nonproductive conformation. The importance of these loops with regard to overall enzymatic activity of the tetramer was revealed by a series of GAC point mutants designed to create a BPTES resistant GAC. | |||
Full-Length Human Glutaminase in Complex with an Allosteric Inhibitor.,Delabarre B, Gross S, Fang C, Gao Y, Jha A, Jiang F, Song J J, Wei W, Hurov JB Biochemistry. 2011 Nov 18. PMID:22049910<ref>PMID:22049910</ref> | |||
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |||
</div> | |||
==See Also== | ==See Also== | ||
*[[Glutaminase|Glutaminase]] | *[[Glutaminase|Glutaminase]] | ||
== References == | |||
== | <references/> | ||
< | __TOC__ | ||
</StructureSection> | |||
[[Category: Glutaminase]] | [[Category: Glutaminase]] | ||
[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Cheng, F | [[Category: Cheng, F]] | ||
[[Category: DeLaBarre, B | [[Category: DeLaBarre, B]] | ||
[[Category: Gao, Y | [[Category: Gao, Y]] | ||
[[Category: Gross, S | [[Category: Gross, S]] | ||
[[Category: Hurov, J B | [[Category: Hurov, J B]] | ||
[[Category: Jha, A | [[Category: Jha, A]] | ||
[[Category: Jiang, F | [[Category: Jiang, F]] | ||
[[Category: Song, J J | [[Category: Song, J J]] | ||
[[Category: Wei, W | [[Category: Wei, W]] | ||
[[Category: Hydrolase-hydrolase inhibitor complex]] | [[Category: Hydrolase-hydrolase inhibitor complex]] | ||
Revision as of 15:24, 9 December 2014
Crystal Structure of Human GAC in Complex with Glutamate and BPTES
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