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6fzm
From Proteopedia
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| - | '''Unreleased structure''' | ||
| - | + | ==Human PARP14 (ARTD8), catalytic fragment in complex with inhibitor ITK6== | |
| + | <StructureSection load='6fzm' size='340' side='right' caption='[[6fzm]], [[Resolution|resolution]] 2.67Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[6fzm]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6FZM OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6FZM FirstGlance]. <br> | ||
| + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=EE5:4-[(8-methyl-4-oxidanylidene-7-prop-1-ynyl-3~{H}-quinazolin-2-yl)methylsulfanyl]benzoic+acid'>EE5</scene></td></tr> | ||
| + | <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[6fym|6fym]]</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=6fzm FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6fzm OCA], [http://pdbe.org/6fzm PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6fzm RCSB], [http://www.ebi.ac.uk/pdbsum/6fzm PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6fzm ProSAT]</span></td></tr> | ||
| + | </table> | ||
| + | == Function == | ||
| + | [[http://www.uniprot.org/uniprot/PAR14_HUMAN PAR14_HUMAN]] Enhances STAT6-dependent transcription (By similarity). Has ADP-ribosyltransferase activity. | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | Poly-ADP-ribose polymerases (PARPs1-16) play pivotal roles in diverse cellular processes. PARPs that catalyze poly-ADP-ribosylation (PARylation) are the best characterized PARP family members because of the availability of potent and selective inhibitors for these PARPs. There has been comparatively little success in developing selective small-molecule inhibitors of PARPs that catalyze mono-ADP-ribosylation (MARylation), limiting our understanding of the cellular role of MARylation. Here we describe the structure-guided design of inhibitors of PARPs that catalyze MARylation. The most selective analog, ITK7, potently inhibits the MARylation activity of PARP11, a nuclear envelope-localized PARP. ITK7 is greater than 200-fold selective over other PARP family members. Using live-cell imaging, we show that ITK7 causes PARP11 to dissociate from the nuclear envelope. These results suggest that the cellular localization of PARP11 is regulated by its catalytic activity. | ||
| - | + | A Potent and Selective PARP11 Inhibitor Suggests Coupling between Cellular Localization and Catalytic Activity.,Kirby IT, Kojic A, Arnold MR, Thorsell AG, Karlberg T, Vermehren-Schmaedick A, Sreenivasan R, Schultz C, Schuler H, Cohen MS Cell Chem Biol. 2018 Dec 20;25(12):1547-1553.e12. doi:, 10.1016/j.chembiol.2018.09.011. Epub 2018 Oct 18. PMID:30344052<ref>PMID:30344052</ref> | |
| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| - | + | </div> | |
| - | + | <div class="pdbe-citations 6fzm" style="background-color:#fffaf0;"></div> | |
| - | + | == References == | |
| - | + | <references/> | |
| - | [[Category: Cohen, M | + | __TOC__ |
| - | + | </StructureSection> | |
| + | [[Category: Cohen, M S]] | ||
[[Category: Karlberg, T]] | [[Category: Karlberg, T]] | ||
| + | [[Category: Kirby, I T]] | ||
| + | [[Category: Schuler, H]] | ||
| + | [[Category: Sreenivasan, R]] | ||
| + | [[Category: Thorsell, A G]] | ||
| + | [[Category: Adp-ribosylation]] | ||
| + | [[Category: Inhibitor complex]] | ||
| + | [[Category: Transferase]] | ||
| + | [[Category: Transferase domain]] | ||
Current revision
Human PARP14 (ARTD8), catalytic fragment in complex with inhibitor ITK6
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