7l9y
From Proteopedia
(Difference between revisions)
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==Human PARP14 (ARTD8), catalytic fragment in complex with RBN012042== | ==Human PARP14 (ARTD8), catalytic fragment in complex with RBN012042== | ||
| - | <StructureSection load='7l9y' size='340' side='right'caption='[[7l9y]]' scene=''> | + | <StructureSection load='7l9y' size='340' side='right'caption='[[7l9y]], [[Resolution|resolution]] 2.25Å' scene=''> |
== Structural highlights == | == Structural highlights == | ||
| - | <table><tr><td colspan='2'>Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7L9Y OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7L9Y FirstGlance]. <br> | + | <table><tr><td colspan='2'>[[7l9y]] is a 4 chain structure with sequence from [https://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7L9Y OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7L9Y FirstGlance]. <br> |
| - | </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=7l9y FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7l9y OCA], [https://pdbe.org/7l9y PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7l9y RCSB], [https://www.ebi.ac.uk/pdbsum/7l9y PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7l9y ProSAT]</span></td></tr> | + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=XRM:7-(cyclopentylamino)-5-fluoro-2-{[(piperidin-4-yl)sulfanyl]methyl}quinazolin-4(3H)-one'>XRM</scene></td></tr> |
| + | <tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">PARP14, BAL2, KIAA1268 ([https://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</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=7l9y FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7l9y OCA], [https://pdbe.org/7l9y PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7l9y RCSB], [https://www.ebi.ac.uk/pdbsum/7l9y PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7l9y ProSAT]</span></td></tr> | ||
</table> | </table> | ||
| + | == Function == | ||
| + | [[https://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 == | ||
| + | PARP14 is an interferon-stimulated gene that is overexpressed in multiple tumor types, influencing pro-tumor macrophage polarization as well as suppressing the antitumor inflammation response by modulating IFN-gamma and IL-4 signaling. PARP14 is a 203 kDa protein that possesses a catalytic domain responsible for the transfer of mono-ADP-ribose to its substrates. PARP14 also contains three macrodomains and a WWE domain which are binding modules for mono-ADP-ribose and poly-ADP-ribose, respectively, in addition to two RNA recognition motifs. Catalytic inhibitors of PARP14 have been shown to reverse IL-4 driven pro-tumor gene expression in macrophages, however it is not clear what roles the non-enzymatic biomolecular recognition motifs play in PARP14-driven immunology and inflammation. To further understand this, we have discovered a heterobifunctional small molecule designed based on a catalytic inhibitor of PARP14 that binds in the enzyme's NAD + -binding site and recruits the E3 ligase cereblon to ubiquitinate it and selectively target it for degradation. | ||
| + | |||
| + | Targeted Degradation of PARP14 Using a Heterobifunctional Small Molecule.,Wigle T, Ren Y, Molina JR, Blackwell DJ, Schenkel LB, Swinger KK, Kuplast-Barr K, Majer CR, Church WD, Lu AZ, Mo J, Abo R, Cheung A, Dorsey BW, Niepel M, Perl NR, Vasbinder MM, Keilhack H, Kuntz KW Chembiochem. 2021 Apr 10. doi: 10.1002/cbic.202100047. PMID:33838082<ref>PMID:33838082</ref> | ||
| + | |||
| + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
| + | </div> | ||
| + | <div class="pdbe-citations 7l9y" style="background-color:#fffaf0;"></div> | ||
| + | == References == | ||
| + | <references/> | ||
__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
| + | [[Category: Human]] | ||
[[Category: Large Structures]] | [[Category: Large Structures]] | ||
| - | [[Category: Church | + | [[Category: Church, W D]] |
| - | [[Category: Dorsey | + | [[Category: Dorsey, B W]] |
| - | [[Category: Kuntz | + | [[Category: Kuntz, K W]] |
| - | [[Category: Perl | + | [[Category: Perl, N R]] |
| - | [[Category: Schenkel | + | [[Category: Schenkel, L B]] |
| - | [[Category: Swinger | + | [[Category: Swinger, K K]] |
| - | [[Category: Vasbinder | + | [[Category: Vasbinder, M M]] |
| - | [[Category: Wigle | + | [[Category: Wigle, T J]] |
| + | [[Category: Adp ribosylation]] | ||
| + | [[Category: Artd8]] | ||
| + | [[Category: Inhibitor complex]] | ||
| + | [[Category: Monoparp]] | ||
| + | [[Category: Parp14]] | ||
| + | [[Category: Transferase]] | ||
| + | [[Category: Transferase-inhibitor complex]] | ||
Revision as of 07:49, 25 June 2021
Human PARP14 (ARTD8), catalytic fragment in complex with RBN012042
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