5eho: Difference between revisions

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'''Unreleased structure'''


The entry 5eho is ON HOLD  until Paper Publication
==Rapid Discovery of Pyrido[3,4-d]pyrimidine Inhibitors of Monopolar Spindle kinase 1 (MPS1) Using a Structure-Based Hydridization Approach==
 
<StructureSection load='5eho' size='340' side='right' caption='[[5eho]], [[Resolution|resolution]] 2.18&Aring;' scene=''>
Authors: Innocenti, P., Woodward, H.L., Solanki, S., Naud, N., Westwood, I.M., Cronin, N., Hayes, A., Roberts, J., Henley, A.T., Baker, R., Faisal, A., Mak, G., Box, G., Valenti, M., De Haven Brandon, A., O'Fee, L., Saville, J., Schmitt, J., Burke, R., van Montfort, R.L.M., Raymaud, F.I., Eccles, S.A., Linardopoulos, S., Blagg, J., Hoelder, S.
== Structural highlights ==
 
<table><tr><td colspan='2'>[[5eho]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5EHO OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5EHO FirstGlance]. <br>
Description: Rapid Discovery of Pyrido[3,4-d]pyrimidine Inhibitors of Monopolar Spindle kinase 1 (MPS1) Using a Structure-Based Hydridization Approach
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=5O1:~{N}8-CYCLOHEXYL-~{N}2-[2-METHOXY-4-(1-METHYLPYRAZOL-4-YL)PHENYL]PYRIDO[3,4-D]PYRIMIDINE-2,8-DIAMINE'>5O1</scene>, <scene name='pdbligand=DMS:DIMETHYL+SULFOXIDE'>DMS</scene></td></tr>
[[Category: Unreleased Structures]]
<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[5eh0|5eh0]]</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=5eho FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5eho OCA], [http://pdbe.org/5eho PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5eho RCSB], [http://www.ebi.ac.uk/pdbsum/5eho PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5eho 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> 
== References ==
<references/>
__TOC__
</StructureSection>
[[Category: Dual-specificity kinase]]
[[Category: Baker, R]]
[[Category: Blagg, J]]
[[Category: Box, G]]
[[Category: Brandon, A De Haven]]
[[Category: Burke, R]]
[[Category: Burke, R]]
[[Category: Van Montfort, R.L.M]]
[[Category: Cronin, N]]
[[Category: Woodward, H.L]]
[[Category: Eccles, S A]]
[[Category: Faisal, A]]
[[Category: Fee, L O]]
[[Category: Hayes, A]]
[[Category: Henley, A T]]
[[Category: Hoelder, S]]
[[Category: Hoelder, S]]
[[Category: Solanki, S]]
[[Category: Innocenti, P]]
[[Category: Innocenti, P]]
[[Category: Hayes, A]]
[[Category: Linardopoulos, S]]
[[Category: Blagg, J]]
[[Category: Westwood, I.M]]
[[Category: Valenti, M]]
[[Category: Mak, G]]
[[Category: Mak, G]]
[[Category: Henley, A.T]]
[[Category: Montfort, R L.M van]]
[[Category: Cronin, N]]
[[Category: Naud, N]]
[[Category: Raymaud, F.I]]
[[Category: Raymaud, F I]]
[[Category: Roberts, J]]
[[Category: Saville, J]]
[[Category: Saville, J]]
[[Category: De Haven Brandon, A]]
[[Category: Eccles, S.A]]
[[Category: Box, G]]
[[Category: Linardopoulos, S]]
[[Category: Schmitt, J]]
[[Category: Schmitt, J]]
[[Category: O'Fee, L]]
[[Category: Solanki, S]]
[[Category: Faisal, A]]
[[Category: Valenti, M]]
[[Category: Baker, R]]
[[Category: Westwood, I M]]
[[Category: Roberts, J]]
[[Category: Woodward, H L]]
[[Category: Naud, N]]
[[Category: Transferase]]

Revision as of 22:45, 9 December 2016

Rapid Discovery of Pyrido[3,4-d]pyrimidine Inhibitors of Monopolar Spindle kinase 1 (MPS1) Using a Structure-Based Hydridization ApproachRapid Discovery of Pyrido[3,4-d]pyrimidine Inhibitors of Monopolar Spindle kinase 1 (MPS1) Using a Structure-Based Hydridization Approach

Structural highlights

5eho is a 1 chain structure. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Ligands:,
Activity:Dual-specificity kinase, with EC number 2.7.12.1
Resources:FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

[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.[1]

References

  1. ↑ Jelluma N, Brenkman AB, van den Broek NJ, Cruijsen CW, van Osch MH, Lens SM, Medema RH, Kops GJ. Mps1 phosphorylates Borealin to control Aurora B activity and chromosome alignment. Cell. 2008 Jan 25;132(2):233-46. doi: 10.1016/j.cell.2007.11.046. PMID:18243099 doi:10.1016/j.cell.2007.11.046

5eho, resolution 2.18Å

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