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6bru

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Current revision (14:49, 4 October 2023) (edit) (undo)
 
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<StructureSection load='6bru' size='340' side='right'caption='[[6bru]], [[Resolution|resolution]] 1.80&Aring;' scene=''>
<StructureSection load='6bru' size='340' side='right'caption='[[6bru]], [[Resolution|resolution]] 1.80&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>[[6bru]] is a 4 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6BRU OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6BRU FirstGlance]. <br>
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<table><tr><td colspan='2'>[[6bru]] is a 4 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=6BRU OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=6BRU FirstGlance]. <br>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=E5M:(7S)-2-[(3,5-difluoro-4-hydroxyphenyl)amino]-5,7,8-trimethyl-7,8-dihydropteridin-6(5H)-one'>E5M</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr>
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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]] 1.8&#8491;</td></tr>
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<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">VRK1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</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=E5M:(7S)-2-[(3,5-difluoro-4-hydroxyphenyl)amino]-5,7,8-trimethyl-7,8-dihydropteridin-6(5H)-one'>E5M</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr>
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<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Non-specific_serine/threonine_protein_kinase Non-specific serine/threonine protein kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.1 2.7.11.1] </span></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=6bru FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6bru OCA], [https://pdbe.org/6bru PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=6bru RCSB], [https://www.ebi.ac.uk/pdbsum/6bru PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=6bru ProSAT]</span></td></tr>
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<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=6bru FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6bru OCA], [http://pdbe.org/6bru PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6bru RCSB], [http://www.ebi.ac.uk/pdbsum/6bru PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6bru ProSAT]</span></td></tr>
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</table>
</table>
== Disease ==
== Disease ==
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[[http://www.uniprot.org/uniprot/VRK1_HUMAN VRK1_HUMAN]] Pontocerebellar hypoplasia type 1. The disease is caused by mutations affecting the gene represented in this entry.
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[https://www.uniprot.org/uniprot/VRK1_HUMAN VRK1_HUMAN] Pontocerebellar hypoplasia type 1. The disease is caused by mutations affecting the gene represented in this entry.
== Function ==
== Function ==
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[[http://www.uniprot.org/uniprot/VRK1_HUMAN VRK1_HUMAN]] Serine/threonine kinase involved in Golgi disassembly during the cell cycle: following phosphorylation by PLK3 during mitosis, required to induce Golgi fragmentation. Acts by mediating phosphorylation of downstream target protein. Phosphorylates 'Thr-18' of p53/TP53 and may thereby prevent the interaction between p53/TP53 and MDM2. Phosphorylates casein and histone H3. Phosphorylates BANF1: disrupts its ability to bind DNA, reduces its binding to LEM domain-containing proteins and causes its relocalization from the nucleus to the cytoplasm. Phosphorylates ATF2 which activates its transcriptional activity.<ref>PMID:10951572</ref> <ref>PMID:14645249</ref> <ref>PMID:15105425</ref> <ref>PMID:16495336</ref> <ref>PMID:18617507</ref> <ref>PMID:19103756</ref>
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[https://www.uniprot.org/uniprot/VRK1_HUMAN VRK1_HUMAN] Serine/threonine kinase involved in Golgi disassembly during the cell cycle: following phosphorylation by PLK3 during mitosis, required to induce Golgi fragmentation. Acts by mediating phosphorylation of downstream target protein. Phosphorylates 'Thr-18' of p53/TP53 and may thereby prevent the interaction between p53/TP53 and MDM2. Phosphorylates casein and histone H3. Phosphorylates BANF1: disrupts its ability to bind DNA, reduces its binding to LEM domain-containing proteins and causes its relocalization from the nucleus to the cytoplasm. Phosphorylates ATF2 which activates its transcriptional activity.<ref>PMID:10951572</ref> <ref>PMID:14645249</ref> <ref>PMID:15105425</ref> <ref>PMID:16495336</ref> <ref>PMID:18617507</ref> <ref>PMID:19103756</ref>
==See Also==
==See Also==
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__TOC__
__TOC__
</StructureSection>
</StructureSection>
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[[Category: Human]]
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[[Category: Homo sapiens]]
[[Category: Large Structures]]
[[Category: Large Structures]]
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[[Category: Non-specific serine/threonine protein kinase]]
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[[Category: Aquino B]]
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[[Category: Aquino, B]]
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[[Category: Arruda P]]
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[[Category: Arruda, P]]
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[[Category: Azevedo A]]
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[[Category: Azevedo, A]]
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[[Category: Counago RM]]
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[[Category: Counago, R M]]
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[[Category: Edwards AM]]
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[[Category: Edwards, A M]]
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[[Category: Elkins JM]]
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[[Category: Elkins, J M]]
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[[Category: Ferreira M]]
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[[Category: Ferreira, M]]
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[[Category: Gama F]]
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[[Category: Gama, F]]
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[[Category: Guimaraes C]]
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[[Category: Guimaraes, C]]
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[[Category: Mascarello A]]
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[[Category: Mascarello, A]]
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[[Category: Massirer KB]]
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[[Category: Massirer, K B]]
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[[Category: De Souza GP]]
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[[Category: Reis, C V.dos]]
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[[Category: Dos Reis CV]]
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[[Category: Structural genomic]]
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[[Category: Souza, G P.de]]
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[[Category: Protein kinase domain]]
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[[Category: Sgc]]
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[[Category: Transferase]]
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[[Category: Transferase-transferase inhbitor complex]]
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[[Category: Transferase-transferase inhibitor complex]]
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Current revision

Crystal Structure of the Human vaccinia-related kinase bound to a (S)-2-phenylaminopteridinone inhibitor

PDB ID 6bru

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