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4b6l

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{{STRUCTURE_4b6l| PDB=4b6l | SCENE= }}
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==Discovery of Oral Polo-Like Kinase (PLK) Inhibitors with Enhanced Selectivity Profile using Residue Targeted Drug Design==
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===Discovery of Oral Polo-Like Kinase (PLK) Inhibitors with Enhanced Selectivity Profile using Residue Targeted Drug Design===
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<StructureSection load='4b6l' size='340' side='right' caption='[[4b6l]], [[Resolution|resolution]] 1.90&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[4b6l]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4B6L OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4B6L 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=9ZP:4-[[(4R)-5-CYCLOPENTYL-4-ETHYL-3A,4-DIHYDRO-3H-[1,2,4]TRIAZOLO[4,3-F]PTERIDIN-7-YL]AMINO]-N-CYCLOPROPYL-3-METHOXY-BENZAMIDE'>9ZP</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/Polo_kinase Polo kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.21 2.7.11.21] </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=4b6l FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4b6l OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4b6l RCSB], [http://www.ebi.ac.uk/pdbsum/4b6l PDBsum]</span></td></tr>
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</table>
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==Function==
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==See Also==
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[[http://www.uniprot.org/uniprot/PLK3_HUMAN PLK3_HUMAN]] Serine/threonine-protein kinase involved in cell cycle regulation, response to stress and Golgi disassembly. Polo-like kinases act by binding and phosphorylating proteins are that already phosphorylated on a specific motif recognized by the POLO box domains. Phosphorylates ATF2, BCL2L1, CDC25A, CDC25C, CHEK2, HIF1A, JUN, p53/TP53, p73/TP73, PTEN, TOP2A and VRK1. Involved in cell cycle regulation: required for entry into S phase and cytokinesis. Phosphorylates BCL2L1, leading to regulate the G2 checkpoint and progression to cytokinesis during mitosis. Plays a key role in response to stress: rapidly activated upon stress stimulation, such as ionizing radiation, reactive oxygen species (ROS), hyperosmotic stress, UV irradiation and hypoxia. Involved in DNA damage response and G1/S transition checkpoint by phosphorylating CDC25A, p53/TP53 and p73/TP73. Phosphorylates p53/TP53 in response to reactive oxygen species (ROS), thereby promoting p53/TP53-mediated apoptosis. Phosphorylates CHEK2 in response to DNA damage, promoting the G2/M transition checkpoint. Phosphorylates the transcription factor p73/TP73 in response to DNA damage, leading to inhibit p73/TP73-mediated transcriptional activation and pro-apoptotic functions. Phosphorylates HIF1A and JUN is response to hypoxia. Phosphorylates ATF2 following hyperosmotic stress in corneal epithelium. Also involved in Golgi disassembly during the cell cycle: part of a MEK1/MAP2K1-dependent pathway that induces Golgi fragmentation during mitosis by mediating phosphorylation of VRK1. May participate in endomitotic cell cycle, a form of mitosis in which both karyokinesis and cytokinesis are interrupted and is a hallmark of megakaryocyte differentiation, via its interaction with CIB1.<ref>PMID:12242661</ref> <ref>PMID:9353331</ref> <ref>PMID:10557092</ref> <ref>PMID:11156373</ref> <ref>PMID:11447225</ref> <ref>PMID:11551930</ref> <ref>PMID:11971976</ref> <ref>PMID:14980500</ref> <ref>PMID:14968113</ref> <ref>PMID:15021912</ref> <ref>PMID:16478733</ref> <ref>PMID:16481012</ref> <ref>PMID:17804415</ref> <ref>PMID:17264206</ref> <ref>PMID:18062778</ref> <ref>PMID:18650425</ref> <ref>PMID:19490146</ref> <ref>PMID:19103756</ref> <ref>PMID:20889502</ref> <ref>PMID:20940307</ref> <ref>PMID:21098032</ref> <ref>PMID:21840391</ref> <ref>PMID:21376736</ref> <ref>PMID:21264284</ref>
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*[[Serine/threonine protein kinase|Serine/threonine protein kinase]]
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__TOC__
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==About this Structure==
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</StructureSection>
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[[4b6l]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4B6L OCA].
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==Reference==
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<references group="xtra"/><references/>
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[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Polo kinase]]
[[Category: Polo kinase]]
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[[Category: Brown, K.]]
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[[Category: Brown, K]]
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[[Category: Charrier, J D.]]
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[[Category: Charrier, J D]]
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[[Category: Durrant, S.]]
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[[Category: Durrant, S]]
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[[Category: Griffiths, M.]]
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[[Category: Griffiths, M]]
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[[Category: Hudson, C.]]
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[[Category: Hudson, C]]
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[[Category: Kay, D.]]
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[[Category: Kay, D]]
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[[Category: Knegtel, R.]]
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[[Category: Knegtel, R]]
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[[Category: ODonnell, M.]]
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[[Category: ODonnell, M]]
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[[Category: Pierard, F.]]
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[[Category: Pierard, F]]
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[[Category: Twin, H.]]
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[[Category: Twin, H]]
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[[Category: Weber, P.]]
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[[Category: Weber, P]]
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[[Category: Young, S.]]
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[[Category: Young, S]]
[[Category: Kinase inhibitor]]
[[Category: Kinase inhibitor]]
[[Category: Transferase]]
[[Category: Transferase]]
[[Category: Water-mediated h-bond]]
[[Category: Water-mediated h-bond]]

Revision as of 09:58, 21 December 2014

Discovery of Oral Polo-Like Kinase (PLK) Inhibitors with Enhanced Selectivity Profile using Residue Targeted Drug Design

4b6l, resolution 1.90Å

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