6ncg

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m (Protected "6ncg" [edit=sysop:move=sysop])
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'''Unreleased structure'''
 
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The entry 6ncg is ON HOLD
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==Crystal Structure of Human Vaccinia-related kinase 2 (VRK-2) bound to pyridin-benzenesulfonamide inhibitor==
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<StructureSection load='6ncg' size='340' side='right' caption='[[6ncg]], [[Resolution|resolution]] 2.45&Aring;' scene=''>
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Authors: dos Reis, C.V., Chiodi, C.G., de Souza, G.P., Guimaraes, C., Mascarello, A., Gama, F., Ferreira, M., Counago, R.M., Massirer, K.B., Elkins, J.M., Arruda, P., Edwards, A.M., Structural Genomics Consortium (SGC)
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== Structural highlights ==
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<table><tr><td colspan='2'>[[6ncg]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6NCG OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6NCG FirstGlance]. <br>
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Description: Crystal Structure of Human Vaccinia-related kinase 2 (VRK-2) bound to pyridin-benzenesulfonamide inhibitor
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=KJD:4-[6-amino-5-(3,5-difluoro-4-hydroxyphenyl)pyridin-3-yl]benzene-1-sulfonamide'>KJD</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr>
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[[Category: Unreleased Structures]]
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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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[[Category: Elkins, J.M]]
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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=6ncg FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6ncg OCA], [http://pdbe.org/6ncg PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6ncg RCSB], [http://www.ebi.ac.uk/pdbsum/6ncg PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6ncg ProSAT]</span></td></tr>
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</table>
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== Function ==
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[[http://www.uniprot.org/uniprot/VRK2_HUMAN VRK2_HUMAN]] Serine/threonine kinase that regulates several signal transduction pathways. Isoform 1 modulates the stress response to hypoxia and cytokines, such as interleukin-1 beta (IL1B) and this is dependent on its interaction with MAPK8IP1, which assembles mitogen-activated protein kinase (MAPK) complexes. Inhibition of signal transmission mediated by the assembly of MAPK8IP1-MAPK complexes reduces JNK phosphorylation and JUN-dependent transcription. Phosphorylates 'Thr-18' of p53/TP53, histone H3, and may also phosphorylate MAPK8IP1. Phosphorylates BANF1 and disrupts its ability to bind DNA and reduces its binding to LEM domain-containing proteins. Downregulates the transactivation of transcription induced by ERBB2, HRAS, BRAF, and MEK1. Blocks the phosphorylation of ERK in response to ERBB2 and HRAS. Can also phosphorylate the following substrates that are commonly used to establish in vitro kinase activity: casein, MBP and histone H2B, but it is not sure that this is physiologically relevant.<ref>PMID:16704422</ref> <ref>PMID:14645249</ref> <ref>PMID:16495336</ref> <ref>PMID:17709393</ref> <ref>PMID:18617507</ref> <ref>PMID:18286207</ref> <ref>PMID:20679487</ref> Isoform 2 phosphorylates 'Thr-18' of p53/TP53, as well as histone H3. Reduces p53/TP53 ubiquitination by MDM2, promotes p53/TP53 acetylation by EP300 and thereby increases p53/TP53 stability and activity.<ref>PMID:16704422</ref> <ref>PMID:14645249</ref> <ref>PMID:16495336</ref> <ref>PMID:17709393</ref> <ref>PMID:18617507</ref> <ref>PMID:18286207</ref> <ref>PMID:20679487</ref>
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== References ==
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<references/>
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__TOC__
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</StructureSection>
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[[Category: Non-specific serine/threonine protein kinase]]
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[[Category: Arruda, P]]
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[[Category: Chiodi, C G]]
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[[Category: Counago, R M]]
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[[Category: Edwards, A M]]
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[[Category: Elkins, J M]]
[[Category: Ferreira, M]]
[[Category: Ferreira, M]]
[[Category: Gama, F]]
[[Category: Gama, F]]
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[[Category: Massirer, K.B]]
 
[[Category: Guimaraes, C]]
[[Category: Guimaraes, C]]
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[[Category: Chiodi, C.G]]
 
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[[Category: Counago, R.M]]
 
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[[Category: De Souza, G.P]]
 
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[[Category: Dos Reis, C.V]]
 
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[[Category: Edwards, A.M]]
 
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[[Category: Arruda, P]]
 
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[[Category: Structural Genomics Consortium (Sgc)]]
 
[[Category: Mascarello, A]]
[[Category: Mascarello, A]]
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[[Category: Massirer, K B]]
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[[Category: Reis, C V.dos]]
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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 inhibitor complex]]

Revision as of 12:15, 16 January 2019

Crystal Structure of Human Vaccinia-related kinase 2 (VRK-2) bound to pyridin-benzenesulfonamide inhibitor

6ncg, resolution 2.45Å

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