5kpp
From Proteopedia
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- | '''Unreleased structure''' | ||
- | + | ==Structure of human PARP1 catalytic domain bound to a quinazoline-2,4(1H,3H)-dione inhibitor== | |
+ | <StructureSection load='5kpp' size='340' side='right'caption='[[5kpp]], [[Resolution|resolution]] 2.33Å' scene=''> | ||
+ | == Structural highlights == | ||
+ | <table><tr><td colspan='2'>[[5kpp]] 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=5KPP OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5KPP 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]] 2.33Å</td></tr> | ||
+ | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=6WZ:1-[[4-FLUORANYL-3-[(3R)-3-METHYL-4-[2,2,2-TRIS(FLUORANYL)ETHYL]PIPERAZIN-1-YL]CARBONYL-PHENYL]METHYL]QUINAZOLINE-2,4-DIONE'>6WZ</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=5kpp FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5kpp OCA], [https://pdbe.org/5kpp PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5kpp RCSB], [https://www.ebi.ac.uk/pdbsum/5kpp PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5kpp ProSAT]</span></td></tr> | ||
+ | </table> | ||
+ | == Function == | ||
+ | [https://www.uniprot.org/uniprot/PARP1_HUMAN PARP1_HUMAN] Involved in the base excision repair (BER) pathway, by catalyzing the poly(ADP-ribosyl)ation of a limited number of acceptor proteins involved in chromatin architecture and in DNA metabolism. This modification follows DNA damages and appears as an obligatory step in a detection/signaling pathway leading to the reparation of DNA strand breaks. Mediates the poly(ADP-ribosyl)ation of APLF and CHFR. Positively regulates the transcription of MTUS1 and negatively regulates the transcription of MTUS2/TIP150. With EEF1A1 and TXK, forms a complex that acts as a T-helper 1 (Th1) cell-specific transcription factor and binds the promoter of IFN-gamma to directly regulate its transcription, and is thus involved importantly in Th1 cytokine production.<ref>PMID:17177976</ref> <ref>PMID:18172500</ref> <ref>PMID:19344625</ref> <ref>PMID:19661379</ref> | ||
- | + | ==See Also== | |
- | + | *[[Poly(ADP-ribose) polymerase 3D structures|Poly(ADP-ribose) polymerase 3D structures]] | |
- | + | == References == | |
- | [[Category: | + | <references/> |
- | [[Category: | + | __TOC__ |
- | [[Category: | + | </StructureSection> |
- | [[Category: | + | [[Category: Homo sapiens]] |
- | [[Category: Xu | + | [[Category: Large Structures]] |
- | [[Category: Zhou | + | [[Category: Cao R]] |
+ | [[Category: Huang N]] | ||
+ | [[Category: Wang YL]] | ||
+ | [[Category: Xu BL]] | ||
+ | [[Category: Zhou J]] |
Current revision
Structure of human PARP1 catalytic domain bound to a quinazoline-2,4(1H,3H)-dione inhibitor
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Categories: Homo sapiens | Large Structures | Cao R | Huang N | Wang YL | Xu BL | Zhou J