4bfp

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{{STRUCTURE_4bfp| PDB=4bfp | SCENE= }}
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==Crystal structure of human tankyrase 2 in complex with WIKI4==
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===Crystal structure of human tankyrase 2 in complex with WIKI4===
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<StructureSection load='4bfp' size='340' side='right' caption='[[4bfp]], [[Resolution|resolution]] 2.40&Aring;' scene=''>
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{{ABSTRACT_PUBMED_23762361}}
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== Structural highlights ==
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<table><tr><td colspan='2'>[[4bfp]] 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=4BFP OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4BFP FirstGlance]. <br>
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</td></tr><tr><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>, <scene name='pdbligand=SWY:2-[3-[[4-(4-METHOXYPHENYL)-5-PYRIDIN-4-YL-1,2,4-TRIAZOL-3-YL]SULFANYL]PROPYL]BENZO[DE]ISOQUINOLINE-1,3-DIONE'>SWY</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene><br>
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<tr><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/NAD(+)_ADP-ribosyltransferase NAD(+) ADP-ribosyltransferase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.4.2.30 2.4.2.30] </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=4bfp FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4bfp OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4bfp RCSB], [http://www.ebi.ac.uk/pdbsum/4bfp PDBsum]</span></td></tr>
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<table>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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Recently a novel inhibitor of Wnt signaling was discovered. The compound, WIKI4, was found to act through tankyrase inhibition and regulate beta-catenin levels in many cancer cell lines and human embryonic stem cells. Here we confirm that WIKI4 is a high potency tankyrase inhibitor and that it selectively inhibits tankyrases over other ARTD enzymes tested. The binding mode of the compound to tankyrase 2 was determined by protein X-ray crystallography to 2.4 A resolution. The structure revealed a novel binding mode to the adenosine subsite of the donor NAD(+) binding groove of the catalytic domain. Our results form a structural basis for further development of potent and selective tankyrase inhibitors based on the WIKI4 scaffold.
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==Function==
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Structural Basis and Selectivity of Tankyrase Inhibition by a Wnt Signaling Inhibitor WIKI4.,Haikarainen T, Venkannagari H, Narwal M, Obaji E, Lee HW, Nkizinkiko Y, Lehtio L PLoS One. 2013 Jun 6;8(6):e65404. doi: 10.1371/journal.pone.0065404. Print 2013. PMID:23762361<ref>PMID:23762361</ref>
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[[http://www.uniprot.org/uniprot/TNKS2_HUMAN TNKS2_HUMAN]] Poly-ADP-ribosyltransferase involved in various processes such as Wnt signaling pathway, telomere length and vesicle trafficking. Acts as an activator of the Wnt signaling pathway by mediating poly-ADP-ribosylation of AXIN1 and AXIN2, 2 key components of the beta-catenin destruction complex: poly-ADP-ribosylated target proteins are recognized by RNF146, which mediates their ubiquitination and subsequent degradation. Also mediates poly-ADP-ribosylation of BLZF1 and CASC3, followed by recruitment of RNF146 and subsequent ubiquitination. Mediates poly-ADP-ribosylation of TERF1, thereby contributing to the regulation of telomere length. May also regulate vesicle trafficking and modulate the subcellular distribution of SLC2A4/GLUT4-vesicles.<ref>PMID:11802774</ref> <ref>PMID:11739745</ref> <ref>PMID:19759537</ref> <ref>PMID:21478859</ref>
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==About this Structure==
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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[[4bfp]] 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=4BFP OCA].
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</div>
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==Reference==
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==See Also==
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<ref group="xtra">PMID:023762361</ref><references group="xtra"/><references/>
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*[[Poly (ADP-ribose) polymerase|Poly (ADP-ribose) polymerase]]
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[[Category: Homo sapiens]]
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== References ==
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<references/>
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__TOC__
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</StructureSection>
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[[Category: Human]]
[[Category: Haikarainen, T.]]
[[Category: Haikarainen, T.]]
[[Category: Lehtio, L.]]
[[Category: Lehtio, L.]]

Revision as of 07:10, 10 September 2014

Crystal structure of human tankyrase 2 in complex with WIKI4

4bfp, resolution 2.40Å

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