4m7b

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(New page: '''Unreleased structure''' The entry 4m7b is ON HOLD Authors: Karlberg, T., Camaioni, E., Schuler, H. Description: HUMAN TANKYRASE 2 -CATALYTIC PARP DOMAIN IN COMPLEX WITH AN INHIBITOR...)
Current revision (16:33, 20 September 2023) (edit) (undo)
 
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'''Unreleased structure'''
 
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The entry 4m7b is ON HOLD
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==Human tankyrase 2 - catalytic Parp domain in complex with an inhibitor UPF1854==
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<StructureSection load='4m7b' size='340' side='right'caption='[[4m7b]], [[Resolution|resolution]] 1.95&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[4m7b]] 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=4M7B OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4M7B 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]] 1.95&#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=28C:4-{2-[(6-METHYL[1,2,4]TRIAZOLO[4,3-B]PYRIDAZIN-8-YL)AMINO]ETHYL}PHENOL'>28C</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</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=4m7b FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4m7b OCA], [https://pdbe.org/4m7b PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4m7b RCSB], [https://www.ebi.ac.uk/pdbsum/4m7b PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4m7b ProSAT]</span></td></tr>
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</table>
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== Function ==
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[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>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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Searching for selective tankyrases (TNKSs) inhibitors, a new small series of 6,8-disubstituted triazolo[4,3-b]piridazines has been synthesized and characterized biologically. Structure-based optimization of the starting hit compound NNL (3) prompted us to the discovery of 4-(2-(6-methyl-[1,2,4]triazolo[4,3-b]pyridazin-8-ylamino)ethyl)phenol (12), a low nanomolar selective TNKSs inhibitor working as NAD isostere as ascertained by crystallographic analysis. Preliminary biological data candidate this new class of derivatives as a powerful pharmacological tools in the unraveling of TNKS implications in physiopathological conditions.
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Authors: Karlberg, T., Camaioni, E., Schuler, H.
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Design, Synthesis, Crystallographic Studies, and Preliminary Biological Appraisal of New Substituted Triazolo[4,3-b]pyridazin-8-amine Derivatives as Tankyrase Inhibitors.,Liscio P, Carotti A, Asciutti S, Karlberg T, Bellocchi D, Llacuna L, Macchiarulo A, Aaronson SA, Schuler H, Pellicciari R, Camaioni E J Med Chem. 2014 Feb 24. PMID:24527792<ref>PMID:24527792</ref>
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Description: HUMAN TANKYRASE 2 -CATALYTIC PARP DOMAIN IN COMPLEX WITH AN INHIBITOR UPF1854
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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</div>
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<div class="pdbe-citations 4m7b" style="background-color:#fffaf0;"></div>
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==See Also==
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*[[Poly(ADP-ribose) polymerase 3D structures|Poly(ADP-ribose) polymerase 3D structures]]
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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: Homo sapiens]]
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[[Category: Large Structures]]
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[[Category: Camaioni E]]
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[[Category: Karlberg T]]
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[[Category: Schuler H]]

Current revision

Human tankyrase 2 - catalytic Parp domain in complex with an inhibitor UPF1854

PDB ID 4m7b

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