2vey: Difference between revisions

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[[Image:2vey.png|left|200px]]


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==CRYSTAL STRUCTURE OF PROTEIN TYROSINE PHOSPHATASE 1B IN COMPLEX WITH AN ISOTHIAZOLIDINONE-CONTAINING INHIBITOR==
The line below this paragraph, containing "STRUCTURE_2vey", creates the "Structure Box" on the page.
<StructureSection load='2vey' size='340' side='right'caption='[[2vey]], [[Resolution|resolution]] 2.20&Aring;' scene=''>
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== Structural highlights ==
or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
<table><tr><td colspan='2'>[[2vey]] 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=2VEY OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2VEY 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]] 2.2&#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=IZ5:N-{(1S)-2-{4-[(5S)-1,1-DIOXIDO-3-OXOISOTHIAZOLIDIN-5-YL]PHENYL}-1-[4-(3-PHENYLPROPYL)-1H-IMIDAZOL-2-YL]ETHYL}-3-FLUOROBENZENESULFONAMIDE'>IZ5</scene></td></tr>
{{STRUCTURE_2vey|  PDB=2vey  |  SCENE= }}
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=2vey FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2vey OCA], [https://pdbe.org/2vey PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2vey RCSB], [https://www.ebi.ac.uk/pdbsum/2vey PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2vey ProSAT]</span></td></tr>
</table>
== Function ==
[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 ==
[[Image:Consurf_key_small.gif|200px|right]]
Check<jmol>
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    <scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/ve/2vey_consurf.spt"</scriptWhenChecked>
    <scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked>
    <text>to colour the structure by Evolutionary Conservation</text>
  </jmolCheckbox>
</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=2vey ConSurf].
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== Publication Abstract from PubMed ==
The structure-based design and synthesis of isothiazolidinone (IZD) inhibitors of PTP1B containing imidazoles and imidazolines and their modification to interact with the B site of PTP1B are described here. The X-ray crystal structures of 3I and 4I complexed with PTP1B were solved and revealed the inhibitors are interacting extensively with the B site of the enzyme.


===CRYSTAL STRUCUTRE OF PROTEIN TYROSINE PHOSPHATASE 1B IN COMPLEX WITH AN ISOTHIAZOLIDINONE-CONTAINING INHIBITOR===
Isothiazolidinone inhibitors of PTP1B containing imidazoles and imidazolines.,Douty B, Wayland B, Ala PJ, Bower MJ, Pruitt J, Bostrom L, Wei M, Klabe R, Gonneville L, Wynn R, Burn TC, Liu PC, Combs AP, Yue EW Bioorg Med Chem Lett. 2008 Jan 1;18(1):66-71. Epub 2007 Nov 9. PMID:18037290<ref>PMID:18037290</ref>


From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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<div class="pdbe-citations 2vey" style="background-color:#fffaf0;"></div>


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==See Also==
The line below this paragraph, {{ABSTRACT_PUBMED_18037290}}, adds the Publication Abstract to the page
*[[Tyrosine phosphatase 3D structures|Tyrosine phosphatase 3D structures]]
(as it appears on PubMed at http://www.pubmed.gov), where 18037290 is the PubMed ID number.
== References ==
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<references/>
{{ABSTRACT_PUBMED_18037290}}
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</StructureSection>
==About this Structure==
2VEY is a 1 chain structure of 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=2VEY OCA].
 
==Reference==
<ref group="xtra">PMID:18037290</ref><references group="xtra"/>
[[Category: Homo sapiens]]
[[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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