2xh1

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<StructureSection load='2xh1' size='340' side='right' caption='[[2xh1]], [[Resolution|resolution]] 2.10&Aring;' scene=''>
<StructureSection load='2xh1' size='340' side='right' caption='[[2xh1]], [[Resolution|resolution]] 2.10&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>[[2xh1]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2XH1 OCA]. <br>
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<table><tr><td colspan='2'>[[2xh1]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2XH1 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2XH1 FirstGlance]. <br>
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</td></tr><tr><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=BF5:(3S)-10-(4-AMINOPIPERAZIN-1-YL)-9-FLUORO-7-HYDROXY-3-METHYL-2,3-DIHYDRO-8H-[1,4]OXAZINO[2,3,4-IJ]QUINOLINE-6-CARBOXYLATE'>BF5</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=IOD:IODIDE+ION'>IOD</scene>, <scene name='pdbligand=PLP:PYRIDOXAL-5-PHOSPHATE'>PLP</scene><br>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=BF5:(3S)-10-(4-AMINOPIPERAZIN-1-YL)-9-FLUORO-7-HYDROXY-3-METHYL-2,3-DIHYDRO-8H-[1,4]OXAZINO[2,3,4-IJ]QUINOLINE-6-CARBOXYLATE'>BF5</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=IOD:IODIDE+ION'>IOD</scene>, <scene name='pdbligand=PLP:PYRIDOXAL-5-PHOSPHATE'>PLP</scene></td></tr>
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<tr><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[2vgz|2vgz]]</td></tr>
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<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[2vgz|2vgz]]</td></tr>
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<tr><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Glucokinase Glucokinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.1.2 2.7.1.2] </span></td></tr>
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<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=2xh1 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2xh1 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=2xh1 RCSB], [http://www.ebi.ac.uk/pdbsum/2xh1 PDBsum]</span></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=2xh1 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2xh1 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=2xh1 RCSB], [http://www.ebi.ac.uk/pdbsum/2xh1 PDBsum]</span></td></tr>
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</table>
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<table>
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== Function ==
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[[http://www.uniprot.org/uniprot/AADAT_HUMAN AADAT_HUMAN]] Transaminase with broad substrate specificity. Has transaminase activity towards aminoadipate, kynurenine, methionine and glutamate. Shows activity also towards tryptophan, aspartate and hydroxykynurenine. Accepts a variety of oxo-acids as amino-group acceptors, with a preference for 2-oxoglutarate, 2-oxocaproic acid, phenylpyruvate and alpha-oxo-gamma-methiol butyric acid. Can also use glyoxylate as amino-group acceptor (in vitro).<ref>PMID:18620547</ref>
== Evolutionary Conservation ==
== Evolutionary Conservation ==
[[Image:Consurf_key_small.gif|200px|right]]
[[Image:Consurf_key_small.gif|200px|right]]
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Crystal structure-based selective targeting of the pyridoxal 5'-phosphate dependent enzyme kynurenine aminotransferase II for cognitive enhancement.,Rossi F, Valentina C, Garavaglia S, Sathyasaikumar KV, Schwarcz R, Kojima S, Okuwaki K, Ono S, Kajii Y, Rizzi M J Med Chem. 2010 Aug 12;53(15):5684-9. PMID:20684605<ref>PMID:20684605</ref>
Crystal structure-based selective targeting of the pyridoxal 5'-phosphate dependent enzyme kynurenine aminotransferase II for cognitive enhancement.,Rossi F, Valentina C, Garavaglia S, Sathyasaikumar KV, Schwarcz R, Kojima S, Okuwaki K, Ono S, Kajii Y, Rizzi M J Med Chem. 2010 Aug 12;53(15):5684-9. PMID:20684605<ref>PMID:20684605</ref>
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
</div>
</div>
== References ==
== References ==
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</StructureSection>
</StructureSection>
[[Category: Human]]
[[Category: Human]]
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[[Category: Casazza, V.]]
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[[Category: Casazza, V]]
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[[Category: Garavaglia, S.]]
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[[Category: Garavaglia, S]]
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[[Category: Kajii, Y.]]
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[[Category: Kajii, Y]]
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[[Category: Kojima, S I.]]
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[[Category: Kojima, S I]]
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[[Category: Okuwaki, K.]]
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[[Category: Okuwaki, K]]
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[[Category: Ono, S I.]]
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[[Category: Ono, S I]]
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[[Category: Rizzi, M.]]
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[[Category: Rizzi, M]]
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[[Category: Rossi, F.]]
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[[Category: Rossi, F]]
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[[Category: Sathyasaikumar, K V.]]
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[[Category: Sathyasaikumar, K V]]
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[[Category: Schwarcz, R.]]
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[[Category: Schwarcz, R]]
[[Category: Covalent inhibition]]
[[Category: Covalent inhibition]]
[[Category: Transferase]]
[[Category: Transferase]]

Revision as of 10:46, 25 December 2014

CRYSTAL STRUCTURE OF HUMAN KAT II-INHIBITOR COMPLEX

2xh1, resolution 2.10Å

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