6f7b
From Proteopedia
(Difference between revisions)
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| - | '''Unreleased structure''' | ||
| - | + | ==Crystal structure of the human Bub1 kinase domain in complex with BAY 1816032== | |
| - | + | <StructureSection load='6f7b' size='340' side='right' caption='[[6f7b]], [[Resolution|resolution]] 2.00Å' scene=''> | |
| - | + | == Structural highlights == | |
| - | + | <table><tr><td colspan='2'>[[6f7b]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6F7B OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6F7B FirstGlance]. <br> | |
| - | + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=CVQ:2-[3,5-bis(fluoranyl)-4-[[3-[5-methoxy-4-[(3-methoxypyridin-4-yl)amino]pyrimidin-2-yl]indazol-1-yl]methyl]phenoxy]ethanol'>CVQ</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene></td></tr> | |
| - | [[Category: | + | <tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=SEP:PHOSPHOSERINE'>SEP</scene></td></tr> |
| + | <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> | ||
| + | <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=6f7b FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6f7b OCA], [http://pdbe.org/6f7b PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6f7b RCSB], [http://www.ebi.ac.uk/pdbsum/6f7b PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6f7b ProSAT]</span></td></tr> | ||
| + | </table> | ||
| + | == Function == | ||
| + | [[http://www.uniprot.org/uniprot/BUB1_HUMAN BUB1_HUMAN]] Serine/threonine-protein kinase that performs 2 crucial functions during mitosis: it is essential for spindle-assembly checkpoint signaling and for correct chromosome alignment. Has a key role in the assembly of checkpoint proteins at the kinetochore, being required for the subsequent localization of CENPF, BUB1B, CENPE and MAD2L1. Required for the kinetochore localization of PLK1. Plays an important role in defining SGOL1 localization and thereby affects sister chromatid cohesion. Acts as a substrate for anaphase-promoting complex or cyclosome (APC/C) in complex with its activator CDH1 (APC/C-Cdh1). Necessary for ensuring proper chromosome segregation and binding to BUB3 is essential for this function. Can regulate chromosome segregation in a kinetochore-independent manner. Can phosphorylate BUB3. The BUB1-BUB3 complex plays a role in the inhibition of APC/C when spindle-assembly checkpoint is activated and inhibits the ubiquitin ligase activity of APC/C by phosphorylating its activator CDC20. This complex can also phosphorylate MAD1L1. Kinase activity is essential for inhibition of APC/CCDC20 and for chromosome alignment but does not play a major role in the spindle-assembly checkpoint activity. Mediates cell death in response to chromosome missegregation and acts to suppress spontaneous tumorigenesis.<ref>PMID:10198256</ref> <ref>PMID:15020684</ref> <ref>PMID:15525512</ref> <ref>PMID:15723797</ref> <ref>PMID:16760428</ref> <ref>PMID:17158872</ref> <ref>PMID:19487456</ref> | ||
| + | == References == | ||
| + | <references/> | ||
| + | __TOC__ | ||
| + | </StructureSection> | ||
| + | [[Category: Non-specific serine/threonine protein kinase]] | ||
| + | [[Category: Ahsen, O von]] | ||
| + | [[Category: Bone, W]] | ||
| + | [[Category: Brands, M]] | ||
| + | [[Category: Briem, H]] | ||
| + | [[Category: Cleve, A]] | ||
| + | [[Category: Fernandez-Montalvan, A]] | ||
| + | [[Category: Hitchcock, M]] | ||
| + | [[Category: Holton, S J]] | ||
| + | [[Category: Johanssen, J]] | ||
| + | [[Category: Mengel, A]] | ||
| + | [[Category: Moenning, U]] | ||
| + | [[Category: Mumberg, D]] | ||
| + | [[Category: Nussbaum, F von]] | ||
| + | [[Category: Prechtl, S]] | ||
| + | [[Category: Puetter, V]] | ||
| + | [[Category: Schroeder, J]] | ||
| + | [[Category: Siemeister, G]] | ||
| + | [[Category: Ziegelbauer, K]] | ||
| + | [[Category: Zitzmann-Kolbe, S]] | ||
| + | [[Category: Bub1]] | ||
| + | [[Category: Kinase inhibitor]] | ||
| + | [[Category: Transferase]] | ||
Revision as of 08:25, 19 December 2018
Crystal structure of the human Bub1 kinase domain in complex with BAY 1816032
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Categories: Non-specific serine/threonine protein kinase | Ahsen, O von | Bone, W | Brands, M | Briem, H | Cleve, A | Fernandez-Montalvan, A | Hitchcock, M | Holton, S J | Johanssen, J | Mengel, A | Moenning, U | Mumberg, D | Nussbaum, F von | Prechtl, S | Puetter, V | Schroeder, J | Siemeister, G | Ziegelbauer, K | Zitzmann-Kolbe, S | Bub1 | Kinase inhibitor | Transferase
