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==CRYSTAL STRUCUTRE OF PROTEIN TYROSINE PHOSPHATASE 1B IN COMPLEX WITH AN ISOTHIAZOLIDINONE-CONTAINING INHIBITOR==
==CRYSTAL STRUCTURE OF PROTEIN TYROSINE PHOSPHATASE 1B IN COMPLEX WITH AN ISOTHIAZOLIDINONE-CONTAINING INHIBITOR==
<StructureSection load='2vex' size='340' side='right' caption='[[2vex]], [[Resolution|resolution]] 2.20&Aring;' scene=''>
<StructureSection load='2vex' size='340' side='right'caption='[[2vex]], [[Resolution|resolution]] 2.20&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
<table><tr><td colspan='2'>[[2vex]] is a 1 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=2VEX OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2VEX FirstGlance]. <br>
<table><tr><td colspan='2'>[[2vex]] 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=2VEX OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2VEX FirstGlance]. <br>
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=IZ4:N-{(1S)-2-{4-[(5S)-1,1-DIOXIDO-3-OXOISOTHIAZOLIDIN-5-YL]PHENYL}-1-[(4R)-4-(2-PHENYLETHYL)-4,5-DIHYDRO-1H-IMIDAZOL-2-YL]ETHYL}-3-FLUOROBENZENESULFONAMIDE'>IZ4</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene></td></tr>
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.2&#8491;</td></tr>
<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[2f6t|2f6t]], [[2f6f|2f6f]], [[2cnf|2cnf]], [[2cm3|2cm3]], [[2cm2|2cm2]], [[1g1f|1g1f]], [[1q6n|1q6n]], [[1ptu|1ptu]], [[1c84|1c84]], [[2veu|2veu]], [[1q1m|1q1m]], [[1nz7|1nz7]], [[2azr|2azr]], [[1c88|1c88]], [[1oet|1oet]], [[1c83|1c83]], [[1sug|1sug]], [[1onz|1onz]], [[1ptv|1ptv]], [[2cnh|2cnh]], [[1xbo|1xbo]], [[1g1g|1g1g]], [[2hnp|2hnp]], [[1t49|1t49]], [[1nwl|1nwl]], [[2f6y|2f6y]], [[2cne|2cne]], [[1nl9|1nl9]], [[1c86|1c86]], [[1kav|1kav]], [[2hnq|2hnq]], [[1jf7|1jf7]], [[1pxh|1pxh]], [[1q6s|1q6s]], [[1l8g|1l8g]], [[2cma|2cma]], [[1q6m|1q6m]], [[1i57|1i57]], [[1bzj|1bzj]], [[1wax|1wax]], [[1ony|1ony]], [[1g1h|1g1h]], [[2cng|2cng]], [[1t4j|1t4j]], [[1kak|1kak]], [[2cni|2cni]], [[2b07|2b07]], [[2cm8|2cm8]], [[1eeo|1eeo]], [[1ptt|1ptt]], [[1g7g|1g7g]], [[1qxk|1qxk]], [[1ecv|1ecv]], [[1oem|1oem]], [[2cmb|2cmb]], [[1nwe|1nwe]], [[2fjn|2fjn]], [[1aax|1aax]], [[2vev|2vev]], [[2vey|2vey]], [[2b4s|2b4s]], [[2bgd|2bgd]], [[2cm7|2cm7]], [[1a5y|1a5y]], [[2cmc|2cmc]], [[1c85|1c85]], [[1lqf|1lqf]], [[1c87|1c87]], [[2f6w|2f6w]], [[1no6|1no6]], [[1pyn|1pyn]], [[2bge|2bge]], [[1oes|1oes]], [[1bzc|1bzc]], [[2f6z|2f6z]], [[2f71|2f71]], [[1q6t|1q6t]], [[1oeu|1oeu]], [[1g7f|1g7f]], [[1nny|1nny]], [[1q6j|1q6j]], [[2f70|2f70]], [[1q6p|1q6p]], [[2f6v|2f6v]], [[1t48|1t48]], [[2fjm|2fjm]], [[1oeo|1oeo]], [[1pa1|1pa1]], [[1ph0|1ph0]], [[1bzh|1bzh]], [[1gfy|1gfy]], [[1een|1een]], [[1pty|1pty]], [[1oev|1oev]]</td></tr>
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=IZ4:N-{(1S)-2-{4-[(5S)-1,1-DIOXIDO-3-OXOISOTHIAZOLIDIN-5-YL]PHENYL}-1-[(4R)-4-(2-PHENYLETHYL)-4,5-DIHYDRO-1H-IMIDAZOL-2-YL]ETHYL}-3-FLUOROBENZENESULFONAMIDE'>IZ4</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene></td></tr>
<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Protein-tyrosine-phosphatase Protein-tyrosine-phosphatase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.1.3.48 3.1.3.48] </span></td></tr>
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=2vex FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2vex OCA], [https://pdbe.org/2vex PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2vex RCSB], [https://www.ebi.ac.uk/pdbsum/2vex PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2vex ProSAT]</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=2vex FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2vex OCA], [http://pdbe.org/2vex PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=2vex RCSB], [http://www.ebi.ac.uk/pdbsum/2vex PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=2vex ProSAT]</span></td></tr>
</table>
</table>
== Function ==
== Function ==
[[http://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>
[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>  
== Evolutionary Conservation ==
== Evolutionary Conservation ==
[[Image:Consurf_key_small.gif|200px|right]]
[[Image:Consurf_key_small.gif|200px|right]]
Check<jmol>
Check<jmol>
   <jmolCheckbox>
   <jmolCheckbox>
     <scriptWhenChecked>select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/ve/2vex_consurf.spt"</scriptWhenChecked>
     <scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/ve/2vex_consurf.spt"</scriptWhenChecked>
     <scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked>
     <scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked>
     <text>to colour the structure by Evolutionary Conservation</text>
     <text>to colour the structure by Evolutionary Conservation</text>
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</div>
</div>
<div class="pdbe-citations 2vex" style="background-color:#fffaf0;"></div>
<div class="pdbe-citations 2vex" style="background-color:#fffaf0;"></div>
==See Also==
*[[Tyrosine phosphatase 3D structures|Tyrosine phosphatase 3D structures]]
== References ==
== References ==
<references/>
<references/>
__TOC__
__TOC__
</StructureSection>
</StructureSection>
[[Category: Human]]
[[Category: Homo sapiens]]
[[Category: Protein-tyrosine-phosphatase]]
[[Category: Large Structures]]
[[Category: Ala, P J]]
[[Category: Ala PJ]]
[[Category: Bostrom, L]]
[[Category: Bostrom L]]
[[Category: Bower, M J]]
[[Category: Bower MJ]]
[[Category: Burn, T C]]
[[Category: Burn TC]]
[[Category: Combs, A P]]
[[Category: Combs AP]]
[[Category: Douty, B]]
[[Category: Douty B]]
[[Category: Gonneville, L]]
[[Category: Gonneville L]]
[[Category: Klabe, R]]
[[Category: Klabe R]]
[[Category: Liu, P C.C]]
[[Category: Liu PCC]]
[[Category: Pruitt, J]]
[[Category: Pruitt J]]
[[Category: Wayland, B]]
[[Category: Wayland B]]
[[Category: Wei, M]]
[[Category: Wei M]]
[[Category: Wynn, R]]
[[Category: Wynn R]]
[[Category: Yue, E W]]
[[Category: Yue EW]]
[[Category: Acetylation]]
[[Category: Endoplasmic reticulum]]
[[Category: Hydrolase]]
[[Category: Membrane]]
[[Category: Oxidation]]
[[Category: Phosphatase]]
[[Category: Phosphorylation]]
[[Category: Polymorphism]]
[[Category: Protein phosphatase]]

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