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3jyj

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{{STRUCTURE_3jyj| PDB=3jyj | SCENE= }}
 
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===Structure-Based Design of Novel PIN1 Inhibitors (II)===
 
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{{ABSTRACT_PUBMED_20207139}}
 
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==Function==
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==Structure-Based Design of Novel PIN1 Inhibitors (II)==
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[[http://www.uniprot.org/uniprot/PIN1_HUMAN PIN1_HUMAN]] Essential PPIase that regulates mitosis presumably by interacting with NIMA and attenuating its mitosis-promoting activity. Displays a preference for an acidic residue N-terminal to the isomerized proline bond. Catalyzes pSer/Thr-Pro cis/trans isomerizations. Down-regulates kinase activity of BTK. Can transactivate multiple oncogenes and induce centrosome amplification, chromosome instability and cell transformation. Required for the efficient dephosphorylation and recycling of RAF1 after mitogen activation.<ref>PMID:15664191</ref><ref>PMID:16644721</ref><ref>PMID:21497122</ref>
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<StructureSection load='3jyj' size='340' side='right'caption='[[3jyj]], [[Resolution|resolution]] 1.87&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[3jyj]] is a 2 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=3JYJ OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3JYJ 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]] 1.87&#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=JZI:(2R,4E)-2-[(NAPHTHALEN-2-YLCARBONYL)AMINO]-5-PHENYLPENT-4-ENOIC+ACID'>JZI</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=3jyj FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3jyj OCA], [https://pdbe.org/3jyj PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3jyj RCSB], [https://www.ebi.ac.uk/pdbsum/3jyj PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3jyj ProSAT]</span></td></tr>
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</table>
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== Function ==
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[https://www.uniprot.org/uniprot/PIN1_HUMAN PIN1_HUMAN] Essential PPIase that regulates mitosis presumably by interacting with NIMA and attenuating its mitosis-promoting activity. Displays a preference for an acidic residue N-terminal to the isomerized proline bond. Catalyzes pSer/Thr-Pro cis/trans isomerizations. Down-regulates kinase activity of BTK. Can transactivate multiple oncogenes and induce centrosome amplification, chromosome instability and cell transformation. Required for the efficient dephosphorylation and recycling of RAF1 after mitogen activation.<ref>PMID:15664191</ref> <ref>PMID:16644721</ref> <ref>PMID:21497122</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/jy/3jyj_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=3jyj ConSurf].
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<div style="clear:both"></div>
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==About this Structure==
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==See Also==
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[[3jyj]] is a 2 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=3JYJ OCA].
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*[[Peptidyl-prolyl cis-trans isomerase 3D structures|Peptidyl-prolyl cis-trans isomerase 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:020207139</ref><references group="xtra"/><references/>
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__TOC__
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</StructureSection>
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: Peptidylprolyl isomerase]]
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[[Category: Large Structures]]
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[[Category: Ferre, R A.]]
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[[Category: Ferre RA]]
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[[Category: Greasley, S E.]]
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[[Category: Greasley SE]]
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[[Category: Cell cycle]]
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[[Category: Isomerase]]
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[[Category: Nucleus]]
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[[Category: Phosphoprotein]]
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[[Category: Ppiase]]
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[[Category: Rotamase]]
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[[Category: Sbdd]]
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[[Category: Small molecule]]
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Current revision

Structure-Based Design of Novel PIN1 Inhibitors (II)

PDB ID 3jyj

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