1xbo

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[[Image:1xbo.png|left|200px]]
 
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{{STRUCTURE_1xbo| PDB=1xbo | SCENE= }}
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==PTP1B complexed with Isoxazole Carboxylic Acid==
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<StructureSection load='1xbo' size='340' side='right'caption='[[1xbo]], [[Resolution|resolution]] 2.50&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[1xbo]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1XBO OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=1XBO 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]] 2.5&#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=IX1:5-(3-{3-[3-HYDROXY-2-(METHOXYCARBONYL)PHENOXY]PROPENYL}PHENYL)-4-(HYDROXYMETHYL)ISOXAZOLE-3-CARBOXYLIC+ACID'>IX1</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=1xbo FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1xbo OCA], [https://pdbe.org/1xbo PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=1xbo RCSB], [https://www.ebi.ac.uk/pdbsum/1xbo PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=1xbo ProSAT]</span></td></tr>
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</table>
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== Function ==
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[https://www.uniprot.org/uniprot/PTN1_HUMAN PTN1_HUMAN] Tyrosine-protein phosphatase which acts as a regulator of endoplasmic reticulum unfolded protein response. Mediates dephosphorylation of EIF2AK3/PERK; inactivating the protein kinase activity of EIF2AK3/PERK. May play an important role in CKII- and p60c-src-induced signal transduction cascades. May regulate the EFNA5-EPHA3 signaling pathway which modulates cell reorganization and cell-cell repulsion.<ref>PMID:21135139</ref> <ref>PMID:22169477</ref>
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== Evolutionary Conservation ==
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[[Image:Consurf_key_small.gif|200px|right]]
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Check<jmol>
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<jmolCheckbox>
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<scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/xb/1xbo_consurf.spt"</scriptWhenChecked>
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<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked>
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<text>to colour the structure by Evolutionary Conservation</text>
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</jmolCheckbox>
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</jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/main_output.php?pdb_ID=1xbo ConSurf].
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<div style="clear:both"></div>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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Guided by X-ray crystallography, we have extended the structure-activity relationship (SAR) study on an isoxazole carboxylic acid-based PTP1B inhibitor (1) and more potent and equally selective (&gt;20-fold selectivity over the highly homologous T-cell PTPase, TCPTP) PTP1B inhibitors were identified. Inhibitor 7 demonstrated good cellular activity against PTP1B in COS 7 cells.
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===PTP1B complexed with Isoxazole Carboxylic Acid===
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Isoxazole carboxylic acids as protein tyrosine phosphatase 1B (PTP1B) inhibitors.,Zhao H, Liu G, Xin Z, Serby MD, Pei Z, Szczepankiewicz BG, Hajduk PJ, Abad-Zapatero C, Hutchins CW, Lubben TH, Ballaron SJ, Haasch DL, Kaszubska W, Rondinone CM, Trevillyan JM, Jirousek MR Bioorg Med Chem Lett. 2004 Nov 15;14(22):5543-6. PMID:15482920<ref>PMID:15482920</ref>
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{{ABSTRACT_PUBMED_15482920}}
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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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==About this Structure==
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<div class="pdbe-citations 1xbo" style="background-color:#fffaf0;"></div>
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[[1xbo]] is a 1 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=1XBO OCA].
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==See Also==
==See Also==
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*[[Tyrosine phosphatase|Tyrosine phosphatase]]
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*[[Tyrosine phosphatase 3D structures|Tyrosine phosphatase 3D structures]]
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== References ==
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==Reference==
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<references/>
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<ref group="xtra">PMID:015482920</ref><references group="xtra"/>
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__TOC__
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</StructureSection>
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: Protein-tyrosine-phosphatase]]
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[[Category: Large Structures]]
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[[Category: Abad-Zapatero, C.]]
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[[Category: Abad-Zapatero C]]
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[[Category: Ballaron, S J.]]
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[[Category: Ballaron SJ]]
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[[Category: Hajduk, P J.]]
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[[Category: Hajduk PJ]]
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[[Category: Hassach, D L.]]
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[[Category: Hassach DL]]
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[[Category: Hutchins, C W.]]
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[[Category: Hutchins CW]]
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[[Category: Jirousek, M R.]]
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[[Category: Jirousek MR]]
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[[Category: Kaszubska, W.]]
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[[Category: Kaszubska W]]
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[[Category: Liu, G.]]
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[[Category: Liu G]]
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[[Category: Lubben, T H.]]
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[[Category: Lubben TH]]
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[[Category: Pei, Z.]]
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[[Category: Pei Z]]
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[[Category: Rondinone, C M.]]
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[[Category: Rondinone CM]]
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[[Category: Serby, M.]]
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[[Category: Serby M]]
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[[Category: Szczepankiewicz, B G.]]
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[[Category: Szczepankiewicz BG]]
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[[Category: Trevillyan, J M.]]
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[[Category: Trevillyan JM]]
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[[Category: Xin, Z.]]
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[[Category: Xin Z]]
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[[Category: Zhao, H.]]
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[[Category: Zhao H]]
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[[Category: Hydrolase]]
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[[Category: Isoxazole carboxylic acid]]
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[[Category: Protein tyrosine phosphatase 1b]]
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[[Category: Ptp1b]]
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Current revision

PTP1B complexed with Isoxazole Carboxylic Acid

PDB ID 1xbo

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