5nqe: Difference between revisions

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'''Unreleased structure'''


The entry 5nqe is ON HOLD
==Human PARP14 (ARTD8), catalytic fragment in complex with an N-aryl piperazine inhibitor==
<StructureSection load='5nqe' size='340' side='right'caption='[[5nqe]], [[Resolution|resolution]] 2.71&Aring;' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>[[5nqe]] 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=5NQE OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5NQE FirstGlance]. <br>
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.71&#8491;</td></tr>
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=94Z:3-[[4-[4-(4-FLUOROPHENYL)PIPERAZIN-1-YL]-4-OXIDANYLIDENE-BUTANOYL]AMINO]BENZAMIDE'>94Z</scene></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=5nqe FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5nqe OCA], [https://pdbe.org/5nqe PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5nqe RCSB], [https://www.ebi.ac.uk/pdbsum/5nqe PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5nqe ProSAT]</span></td></tr>
</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 ==
A series of (Z)-4-(3-carbamoylphenylamino)-4-oxobut-2-enyl amides were synthesized and tested for their ability to inhibit the mono-(ADP-ribosyl)transferase, PARP14 (a.k.a. BAL-2; ARTD-8). Two synthetic routes were established for this series and several compounds were identified as sub-micromolar inhibitors of PARP14, the most potent of which was compound 4t, IC50=160nM. Furthermore, profiling other members of this series identified compounds with &gt;20-fold selectivity over PARP5a/TNKS1, and modest selectivity over PARP10, a closely related mono-(ADP-ribosyl)transferase.


Authors: Karlberg, T., Thorsell, A.G., Schuler, H.
Design and synthesis of potent inhibitors of the mono(ADP-ribosyl)transferase, PARP14.,Upton K, Meyers M, Thorsell AG, Karlberg T, Holechek J, Lease R, Schey G, Wolf E, Lucente A, Schuler H, Ferraris D Bioorg Med Chem Lett. 2017 Apr 29. pii: S0960-894X(17)30473-0. doi:, 10.1016/j.bmcl.2017.04.089. PMID:28495083<ref>PMID:28495083</ref>


Description: Human PARP14 (ARTD8), catalytic fragment in complex with an N-aryl piperazine inhibitor
From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
[[Category: Unreleased Structures]]
</div>
[[Category: Thorsell, A.G]]
<div class="pdbe-citations 5nqe" style="background-color:#fffaf0;"></div>
[[Category: Schuler, H]]
 
[[Category: Karlberg, T]]
==See Also==
*[[Poly(ADP-ribose) polymerase 3D structures|Poly(ADP-ribose) polymerase 3D structures]]
== References ==
<references/>
__TOC__
</StructureSection>
[[Category: Homo sapiens]]
[[Category: Large Structures]]
[[Category: Karlberg T]]
[[Category: Schuler H]]
[[Category: Thorsell AG]]
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