View source for 6gvj


==Human Mps1 kinase domain with ordered activation loop==
<StructureSection load='6gvj' size='340' side='right'caption='[[6gvj]], [[Resolution|resolution]] 2.41&Aring;' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>[[6gvj]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6GVJ OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6GVJ FirstGlance]. <br>
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene></td></tr>
<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">TTK, MPS1, MPS1L1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr>
<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Dual-specificity_kinase Dual-specificity kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.12.1 2.7.12.1] </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=6gvj FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6gvj OCA], [http://pdbe.org/6gvj PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6gvj RCSB], [http://www.ebi.ac.uk/pdbsum/6gvj PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6gvj ProSAT]</span></td></tr>
</table>
== Function ==
[[http://www.uniprot.org/uniprot/TTK_HUMAN TTK_HUMAN]] Phosphorylates proteins on serine, threonine, and tyrosine. Probably associated with cell proliferation. Essential for chromosome alignment by enhancing AURKB activity (via direct CDCA8 phosphorylation) at the centromere, and for the mitotic checkpoint.<ref>PMID:18243099</ref>  
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
Monopolar spindle 1 (Mps1) is a dual-specificity protein kinase, orchestrating faithful chromosome segregation during mitosis. All reported structures of the Mps1 kinase adopt the hallmarks of an inactive conformation, which includes a mostly disordered activation loop. Here we present a 2.4A resolution crystal structure of an 'extended' version of the Mps1 kinase domain, which shows an ordered activation loop. However, the other structural characteristics of an active kinase are not present. Our structure shows that the Mps1 activation loop can fit to the ATP binding pocket and interferes with ATP, but less so with inhibitors binding, partly explain the potency of various Mps1 inhibitors. This article is protected by copyright. All rights reserved.

A crystal structure of the human protein kinase Mps1 reveals an ordered conformation of the activation loop.,Roorda JC, Joosten RP, Perrakis A, Hiruma Y Proteins. 2018 Dec 23. doi: 10.1002/prot.25651. PMID:30582207<ref>PMID:30582207</ref>

From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
</div>
<div class="pdbe-citations 6gvj" style="background-color:#fffaf0;"></div>
== References ==
<references/>
__TOC__
</StructureSection>
[[Category: Dual-specificity kinase]]
[[Category: Human]]
[[Category: Large Structures]]
[[Category: Hiruma, Y]]
[[Category: Joosten, R P]]
[[Category: Perrakis, A]]
[[Category: Roorda, J C]]
[[Category: Activation loop]]
[[Category: Activation segment]]
[[Category: Kinase]]
[[Category: Mitosis checkpoint]]
[[Category: Mps1]]
[[Category: Transferase]]
[[Category: Ttk]]