4cqg

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==The crystal structure of MPK38 in complex with OTSSP167, an orally- administrative MELK selective inhibitor==
==The crystal structure of MPK38 in complex with OTSSP167, an orally- administrative MELK selective inhibitor==
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<StructureSection load='4cqg' size='340' side='right' caption='[[4cqg]], [[Resolution|resolution]] 2.57&Aring;' scene=''>
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<StructureSection load='4cqg' size='340' side='right'caption='[[4cqg]], [[Resolution|resolution]] 2.57&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>[[4cqg]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4CQG OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4CQG FirstGlance]. <br>
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<table><tr><td colspan='2'>[[4cqg]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Mus_musculus Mus musculus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4CQG OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4CQG FirstGlance]. <br>
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</td></tr><tr><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=OT5:1-[6-(3,5-DICHLORO-4-HYDROXYPHENYL)-4-({TRANS-4-[(DIMETHYLAMINO)METHYL]CYCLOHEXYL}AMINO)-1,5-NAPHTHYRIDIN-3-YL]ETHANONE'>OT5</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene><br>
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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]] 2.57&#8491;</td></tr>
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<tr><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4cqg FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4cqg OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4cqg RCSB], [http://www.ebi.ac.uk/pdbsum/4cqg PDBsum]</span></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=OT5:1-[6-(3,5-DICHLORO-4-HYDROXYPHENYL)-4-({TRANS-4-[(DIMETHYLAMINO)METHYL]CYCLOHEXYL}AMINO)-1,5-NAPHTHYRIDIN-3-YL]ETHANONE'>OT5</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr>
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<table>
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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=4cqg FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4cqg OCA], [https://pdbe.org/4cqg PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4cqg RCSB], [https://www.ebi.ac.uk/pdbsum/4cqg PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4cqg ProSAT]</span></td></tr>
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</table>
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== Function ==
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[https://www.uniprot.org/uniprot/MELK_MOUSE MELK_MOUSE] Serine/threonine-protein kinase involved in various processes such as cell cycle regulation, self-renewal of stem cells, apoptosis and splicing regulation. Has a broad substrate specificity; phosphorylates BCL2L14, CDC25B, MAP3K5/ASK1 and ZNF622. Acts as an activator of apoptosis by phosphorylating and activating MAP3K5/ASK1. Acts as a regulator of cell cycle, notably by mediating phosphorylation of CDC25B, promoting localization of CDC25B to the centrosome and the spindle poles during mitosis. Plays a key role in cell proliferation. Required for proliferation of embryonic and postnatal multipotent neural progenitors. Phosphorylates and inhibits BCL2L14. Also involved in the inhibition of spliceosome assembly during mitosis by phosphorylating ZNF622, thereby contributing to its redirection to the nucleus. May also play a role in primitive hematopoiesis.<ref>PMID:16061694</ref> <ref>PMID:18948261</ref>
<div style="background-color:#fffaf0;">
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
== Publication Abstract from PubMed ==
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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</div>
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<div class="pdbe-citations 4cqg" style="background-color:#fffaf0;"></div>
== References ==
== References ==
<references/>
<references/>
__TOC__
__TOC__
</StructureSection>
</StructureSection>
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[[Category: Cho, H S.]]
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[[Category: Large Structures]]
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[[Category: Cho, Y S.]]
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[[Category: Mus musculus]]
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[[Category: Kang, Y J.]]
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[[Category: Cho HS]]
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[[Category: Transferase]]
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[[Category: Cho YS]]
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[[Category: Kang YJ]]

Current revision

The crystal structure of MPK38 in complex with OTSSP167, an orally- administrative MELK selective inhibitor

PDB ID 4cqg

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