4i5m

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m (Protected "4i5m" [edit=sysop:move=sysop])
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'''Unreleased structure'''
 
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The entry 4i5m is ON HOLD
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==Selective & Brain-Permeable Polo-like Kinase-2 (Plk-2) Inhibitors that Reduce -Synuclein Phosphorylation in Rat Brain==
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<StructureSection load='4i5m' size='340' side='right'caption='[[4i5m]], [[Resolution|resolution]] 1.80&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[4i5m]] is a 1 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=4I5M OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4I5M FirstGlance]. <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]] 1.801&#8491;</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=R78:4-{[(7R)-8-CYCLOPENTYL-7-ETHYL-5-METHYL-6-OXO-5,6,7,8-TETRAHYDROPTERIDIN-2-YL]AMINO}-3-METHOXY-N-(1-METHYLPIPERIDIN-4-YL)BENZAMIDE'>R78</scene></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=4i5m FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4i5m OCA], [https://pdbe.org/4i5m PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4i5m RCSB], [https://www.ebi.ac.uk/pdbsum/4i5m PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4i5m ProSAT]</span></td></tr>
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</table>
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== Function ==
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[https://www.uniprot.org/uniprot/PLK2_HUMAN PLK2_HUMAN] Tumor suppressor serine/threonine-protein kinase involved in synaptic plasticity, centriole duplication and G1/S phase transition. Polo-like kinases act by binding and phosphorylating proteins are that already phosphorylated on a specific motif recognized by the POLO box domains. Phosphorylates CENPJ, NPM1, RAPGEF2, RASGRF1, SNCA, SIPA1L1 and SYNGAP1. Plays a key role in synaptic plasticity and memory by regulating the Ras and Rap protein signaling: required for overactivity-dependent spine remodeling by phosphorylating the Ras activator RASGRF1 and the Rap inhibitor SIPA1L1 leading to their degradation by the proteasome. Conversely, phosphorylates the Rap activator RAPGEF2 and the Ras inhibitor SYNGAP1, promoting their activity. Also regulates synaptic plasticity independently of kinase activity, via its interaction with NSF that disrupts the interaction between NSF and the GRIA2 subunit of AMPARs, leading to a rapid rundown of AMPAR-mediated current that occludes long term depression. Required for procentriole formation and centriole duplication by phosphorylating CENPJ and NPM1, respectively. Its induction by p53/TP53 suggests that it may participate in the mitotic checkpoint following stress.<ref>PMID:15242618</ref> <ref>PMID:19001868</ref> <ref>PMID:20531387</ref> <ref>PMID:20352051</ref>
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Authors: Aubele, D.L., Hom, R.K., Adler, M., Galemmo, Jr., R.A., Bowers, S., Truong, A.P., Pan, H., Beroza, P., Neitz, R.J., Yao, N., Lin, M., Tonn, G., Zhang, H., Bova, M.P., Ren, Z., Tam, D., Ruslim, L., Baker, J., Diep, L., Fitzgerald, K., Hoffman, J., Motter, R., Fauss, D., Tanaka, P., Dappen, M., Jagodzinski, J., Chan, W., Konradi, A.W., Latimer, L., Zhu, Y.L., Artis, D.R., Sham, H.L., Anderson, J.P., Bergeron, M.
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==See Also==
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*[[Serine/threonine protein kinase 3D structures|Serine/threonine protein kinase 3D structures]]
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Description: Selective & Brain-Permeable Polo-like Kinase-2 (Plk-2) Inhibitors that Reduce -Synuclein Phosphorylation in Rat Brain
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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: Homo sapiens]]
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[[Category: Large Structures]]
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[[Category: Adler M]]
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[[Category: Anderson JP]]
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[[Category: Artis DR]]
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[[Category: Aubele DL]]
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[[Category: Baker J]]
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[[Category: Bergeron M]]
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[[Category: Beroza P]]
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[[Category: Bova MP]]
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[[Category: Bowers S]]
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[[Category: Chan W]]
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[[Category: Dappen M]]
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[[Category: Diep L]]
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[[Category: Fauss D]]
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[[Category: Fitzgerald K]]
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[[Category: Galemmo Jr RA]]
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[[Category: Hoffman J]]
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[[Category: Hom RK]]
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[[Category: Jagodzinski J]]
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[[Category: Konradi AW]]
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[[Category: Latimer L]]
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[[Category: Lin M]]
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[[Category: Motter R]]
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[[Category: Neitz RJ]]
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[[Category: Pan H]]
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[[Category: Ren Z]]
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[[Category: Ruslim L]]
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[[Category: Sham HL]]
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[[Category: Tam D]]
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[[Category: Tanaka P]]
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[[Category: Tonn G]]
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[[Category: Truong AP]]
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[[Category: Yao N]]
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[[Category: Zhang H]]
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[[Category: Zhu YL]]

Current revision

Selective & Brain-Permeable Polo-like Kinase-2 (Plk-2) Inhibitors that Reduce -Synuclein Phosphorylation in Rat Brain

PDB ID 4i5m

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