6rch

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m (Protected "6rch" [edit=sysop:move=sysop])
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'''Unreleased structure'''
 
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The entry 6rch is ON HOLD
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==Crystal structure of Casein kinase I isoform delta (CK1 delta) complexed with SR4133 inhibitor==
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<StructureSection load='6rch' size='340' side='right'caption='[[6rch]], [[Resolution|resolution]] 1.45&Aring;' scene=''>
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Authors: Chaikuad, A., Arrowsmith, C.H., Edwards, A.M., Bountra, C., Roush, W.R., Knapp, S., Structural Genomics Consortium (SGC)
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== Structural highlights ==
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<table><tr><td colspan='2'>[[6rch]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6RCH OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6RCH FirstGlance]. <br>
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Description: Crystal structure of Casein kinase I isoform delta (CK1 delta) complexed with SR4133 inhibitor
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=K0B:~{N}-[[4,5-bis(fluoranyl)-1~{H}-benzimidazol-2-yl]methyl]-2-morpholin-4-yl-9-naphthalen-2-yl-purin-6-amine'>K0B</scene>, <scene name='pdbligand=NA:SODIUM+ION'>NA</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr>
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[[Category: Unreleased Structures]]
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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=6rch FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6rch OCA], [http://pdbe.org/6rch PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6rch RCSB], [http://www.ebi.ac.uk/pdbsum/6rch PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6rch ProSAT]</span></td></tr>
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</table>
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== Disease ==
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[[http://www.uniprot.org/uniprot/KC1D_HUMAN KC1D_HUMAN]] Familial advanced sleep-phase syndrome. The disease is caused by mutations affecting the gene represented in this entry.
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== Function ==
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[[http://www.uniprot.org/uniprot/KC1D_HUMAN KC1D_HUMAN]] Essential serine/threonine-protein kinase that regulates diverse cellular growth and survival processes including Wnt signaling, DNA repair and circadian rhythms. It can phosphorylate a large number of proteins. Casein kinases are operationally defined by their preferential utilization of acidic proteins such as caseins as substrates. Phosphorylates connexin-43/GJA1, MAP1A, SNAPIN, MAPT/TAU, TOP2A, DCK, HIF1A, EIF6, p53/TP53, DVL2, DVL3, ESR1, AIB1/NCOA3, DNMT1, PKD2, YAP1, PER1 and PER2. Central component of the circadian clock. May act as a negative regulator of circadian rhythmicity by phosphorylating PER1 and PER2, leading to retain PER1 in the cytoplasm. YAP1 phosphorylation promotes its SCF(beta-TRCP) E3 ubiquitin ligase-mediated ubiquitination and subsequent degradation. DNMT1 phosphorylation reduces its DNA-binding activity. Phosphorylation of ESR1 and AIB1/NCOA3 stimulates their activity and coactivation. Phosphorylation of DVL2 and DVL3 regulates WNT3A signaling pathway that controls neurite outgrowth. EIF6 phosphorylation promotes its nuclear export. Triggers down-regulation of dopamine receptors in the forebrain. Activates DCK in vitro by phosphorylation. TOP2A phosphorylation favors DNA cleavable complex formation. May regulate the formation of the mitotic spindle apparatus in extravillous trophoblast. Modulates connexin-43/GJA1 gap junction assembly by phosphorylation. Probably involved in lymphocyte physiology. Regulates fast synaptic transmission mediated by glutamate.<ref>PMID:10606744</ref> <ref>PMID:12270943</ref> <ref>PMID:14761950</ref> <ref>PMID:16027726</ref> <ref>PMID:17962809</ref> <ref>PMID:17562708</ref> <ref>PMID:19043076</ref> <ref>PMID:19339517</ref> <ref>PMID:20637175</ref> <ref>PMID:20041275</ref> <ref>PMID:20048001</ref> <ref>PMID:20699359</ref> <ref>PMID:20696890</ref> <ref>PMID:20407760</ref> <ref>PMID:21084295</ref> <ref>PMID:21422228</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: Large Structures]]
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[[Category: Arrowsmith, C H]]
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[[Category: Bountra, C]]
[[Category: Chaikuad, A]]
[[Category: Chaikuad, A]]
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[[Category: Arrowsmith, C.H]]
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[[Category: Edwards, A M]]
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[[Category: Roush, W.R]]
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[[Category: Knapp, S]]
[[Category: Knapp, S]]
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[[Category: Edwards, A.M]]
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[[Category: Roush, W R]]
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[[Category: Structural Genomics Consortium (Sgc)]]
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[[Category: Structural genomic]]
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[[Category: Bountra, C]]
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[[Category: Ck1 delta]]
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[[Category: Ck1d]]
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[[Category: Kinase inhibitor]]
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[[Category: Sgc]]
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[[Category: Transferase]]

Revision as of 10:16, 27 March 2020

Crystal structure of Casein kinase I isoform delta (CK1 delta) complexed with SR4133 inhibitor

PDB ID 6rch

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