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5lxp

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'''Unreleased structure'''
 
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The entry 5lxp is ON HOLD
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==Human PARP14 (ARTD8), catalytic fragment in complex with inhibitor H5==
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<StructureSection load='5lxp' size='340' side='right'caption='[[5lxp]], [[Resolution|resolution]] 2.07&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[5lxp]] 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=5LXP OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5LXP 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]] 2.07&#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=7AG:~{N}-(3-AMINOCARBONYLPHENYL)-~{N}-[[1-[(2~{R})-2-PHENYLPROPYL]-1,2,3-TRIAZOL-4-YL]METHYL]PENTANEDIAMIDE'>7AG</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=5lxp FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5lxp OCA], [https://pdbe.org/5lxp PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5lxp RCSB], [https://www.ebi.ac.uk/pdbsum/5lxp PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5lxp ProSAT]</span></td></tr>
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</table>
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== Function ==
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[https://www.uniprot.org/uniprot/PAR14_HUMAN PAR14_HUMAN] Enhances STAT6-dependent transcription (By similarity). Has ADP-ribosyltransferase activity.
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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Poly(ADP-ribose) polymerases (PARPs) are key enzymes in a variety of cellular processes. Most small-molecule PARP inhibitors developed to date have been against PARP1, and suffer from poor selectivity. PARP14 has recently emerged as a potential therapeutic target, but its inhibitor development has trailed behind. Herein, we describe a small molecule microarray-based strategy for high-throughput synthesis, screening of &gt;1000 potential bidentate inhibitors of PARPs, and the successful discovery of a potent PARP14 inhibitor H10 with &gt;20-fold selectivity over PARP1. Co-crystallization of the PARP14/H10 complex indicated H10 bound to both the nicotinamide and the adenine subsites. Further structure-activity relationship studies identified important binding elements in the adenine subsite. In tumor cells, H10 was able to chemically knockdown endogenous PARP14 activities.
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Authors: Karlberg, T., Thorsell, A.G., Schuler, H.
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Small Molecule Microarray Based Discovery of PARP14 Inhibitors.,Peng B, Thorsell AG, Karlberg T, Schuler H, Yao SQ Angew Chem Int Ed Engl. 2016 Dec 5. doi: 10.1002/anie.201609655. PMID:27918638<ref>PMID:27918638</ref>
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Description: Human PARP14 (ARTD8), catalytic fragment in complex with inhibitor H5
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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[[Category: Unreleased Structures]]
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</div>
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[[Category: Thorsell, A.G]]
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<div class="pdbe-citations 5lxp" style="background-color:#fffaf0;"></div>
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[[Category: Karlberg, T]]
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[[Category: Schuler, H]]
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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: Karlberg T]]
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[[Category: Schuler H]]
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[[Category: Thorsell AG]]

Current revision

Human PARP14 (ARTD8), catalytic fragment in complex with inhibitor H5

PDB ID 5lxp

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