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==Structural basis and SAR for OD 270, a lead stage 1,2,4-triazole based specific Tankyrase1/2 inhibitor==
==Structural basis and SAR for OD 270, a lead stage 1,2,4-triazole based specific Tankyrase1/2 inhibitor==
<StructureSection load='4hyf' size='340' side='right' caption='[[4hyf]], [[Resolution|resolution]] 2.80&Aring;' scene=''>
<StructureSection load='4hyf' size='340' side='right'caption='[[4hyf]], [[Resolution|resolution]] 2.80&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
<table><tr><td colspan='2'>[[4hyf]] is a 3 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=4HYF OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4HYF FirstGlance]. <br>
<table><tr><td colspan='2'>[[4hyf]] is a 3 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=4HYF OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4HYF FirstGlance]. <br>
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=1AK:4-{5-[(E)-2-{4-(2-CHLOROPHENYL)-5-[5-(METHYLSULFONYL)PYRIDIN-2-YL]-4H-1,2,4-TRIAZOL-3-YL}ETHENYL]-1,3,4-OXADIAZOL-2-YL}BENZONITRILE'>1AK</scene>, <scene name='pdbligand=NCA:NICOTINAMIDE'>NCA</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</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]] 2.8&#8491;</td></tr>
<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[3kr8|3kr8]], [[3kr7|3kr7]], [[4hkn|4hkn]], [[3u9y|3u9y]], [[3p0n|3p0n]], [[4hki|4hki]]</td></tr>
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=1AK:4-{5-[(E)-2-{4-(2-CHLOROPHENYL)-5-[5-(METHYLSULFONYL)PYRIDIN-2-YL]-4H-1,2,4-TRIAZOL-3-YL}ETHENYL]-1,3,4-OXADIAZOL-2-YL}BENZONITRILE'>1AK</scene>, <scene name='pdbligand=NCA:NICOTINAMIDE'>NCA</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr>
<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">PARP5B, TANK2, TNKL, TNKS2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])</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=4hyf FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4hyf OCA], [https://pdbe.org/4hyf PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4hyf RCSB], [https://www.ebi.ac.uk/pdbsum/4hyf PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4hyf ProSAT]</span></td></tr>
<tr id='activity'><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>
<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=4hyf FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4hyf OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4hyf RCSB], [http://www.ebi.ac.uk/pdbsum/4hyf PDBsum]</span></td></tr>
</table>
</table>
== Function ==
== Function ==
[[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>
[https://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>  
<div style="background-color:#fffaf0;">
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
== Publication Abstract from PubMed ==
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
</div>
</div>
<div class="pdbe-citations 4hyf" style="background-color:#fffaf0;"></div>


==See Also==
==See Also==
*[[Poly (ADP-ribose) polymerase|Poly (ADP-ribose) polymerase]]
*[[Poly(ADP-ribose) polymerase 3D structures|Poly(ADP-ribose) polymerase 3D structures]]
== References ==
== References ==
<references/>
<references/>
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</StructureSection>
</StructureSection>
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Drewes, G]]
[[Category: Large Structures]]
[[Category: Ekblad, B]]
[[Category: Drewes G]]
[[Category: Holsworth, D D]]
[[Category: Ekblad B]]
[[Category: Krauss, S]]
[[Category: Holsworth DD]]
[[Category: Morth, J P]]
[[Category: Krauss S]]
[[Category: Perdreau, H]]
[[Category: Morth JP]]
[[Category: Schueler, H]]
[[Category: Perdreau H]]
[[Category: Voronkov, A]]
[[Category: Schueler H]]
[[Category: Waaler, J]]
[[Category: Voronkov A]]
[[Category: Adp-ribosylation]]
[[Category: Waaler J]]
[[Category: Ank repeat]]
[[Category: Catalytic fragment]]
[[Category: Chromosomal protein]]
[[Category: Glycosyltransferase]]
[[Category: Parp]]
[[Category: Phosphorylation]]
[[Category: Telomere]]
[[Category: Transferase]]
[[Category: Transferase-transferase inhibitor complex]]
[[Category: Translocation]]
[[Category: Transport]]
[[Category: Wnt-signalling]]
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