View source for 9rj2


==Bub1 kinase domain in complex with covalent inhibitor BM047==
<StructureSection load='9rj2' size='340' side='right'caption='[[9rj2]], [[Resolution|resolution]] 2.30&Aring;' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>[[9rj2]] is a 2 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=9RJ2 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=9RJ2 FirstGlance]. <br>
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.3&#8491;</td></tr>
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=A1JG6:(2~{R})-~{N}-[4-[(3-chloranyl-4-fluoranyl-phenyl)amino]-7-prop-2-ynoxy-quinazolin-6-yl]-1-(2-fluoranylethanoyl)pyrrolidine-2-carboxamide'>A1JG6</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=SEP:PHOSPHOSERINE'>SEP</scene></td></tr>
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=9rj2 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=9rj2 OCA], [https://pdbe.org/9rj2 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=9rj2 RCSB], [https://www.ebi.ac.uk/pdbsum/9rj2 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=9rj2 ProSAT]</span></td></tr>
</table>
== Function ==
[https://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/>
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</StructureSection>
[[Category: Homo sapiens]]
[[Category: Large Structures]]
[[Category: Ahmad MUD]]
[[Category: Konijnenberg MJ]]
[[Category: Perrakis A]]