2x9e

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[[Image:2x9e.png|left|200px]]
 
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{{STRUCTURE_2x9e| PDB=2x9e | SCENE= }}
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==HUMAN MPS1 IN COMPLEX WITH NMS-P715==
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<StructureSection load='2x9e' size='340' side='right'caption='[[2x9e]], [[Resolution|resolution]] 3.10&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[2x9e]] is a 1 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=2X9E OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2X9E FirstGlance]. <br>
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</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 3.1&#8491;</td></tr>
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=SVE:N-(2,6-DIETHYLPHENYL)-1-METHYL-8-({4-[(1-METHYLPIPERIDIN-4-YL)CARBAMOYL]-2-(TRIFLUOROMETHOXY)PHENYL}AMINO)-4,5-DIHYDRO-1H-PYRAZOLO[4,3-H]QUINAZOLINE-3-CARBOXAMIDE'>SVE</scene></td></tr>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=2x9e FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2x9e OCA], [https://pdbe.org/2x9e PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2x9e RCSB], [https://www.ebi.ac.uk/pdbsum/2x9e PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2x9e ProSAT]</span></td></tr>
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</table>
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== Function ==
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[https://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>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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MPS1 kinase is a key regulator of the spindle assembly checkpoint (SAC), a mitotic mechanism specifically required for proper chromosomal alignment and segregation. It has been found aberrantly overexpressed in a wide range of human tumors and is necessary for tumoral cell proliferation. Here we report the identification and characterization of NMS-P715, a selective and orally bioavailable MPS1 small-molecule inhibitor, which selectively reduces cancer cell proliferation, leaving normal cells almost unaffected. NMS-P715 accelerates mitosis and affects kinetochore components localization causing massive aneuploidy and cell death in a variety of tumoral cell lines and inhibits tumor growth in preclinical cancer models. Inhibiting the SAC could represent a promising new approach to selectively target cancer cells. Cancer Res; 70(24); 10255-64. (c)2010 AACR.
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===HUMAN MPS1 IN COMPLEX WITH NMS-P715===
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Targeting the Mitotic Checkpoint for Cancer Therapy with NMS-P715, an Inhibitor of MPS1 Kinase.,Colombo R, Caldarelli M, Mennecozzi M, Giorgini ML, Sola F, Cappella P, Perrera C, Depaolini SR, Rusconi L, Cucchi U, Avanzi N, Bertrand JA, Bossi RT, Pesenti E, Galvani A, Isacchi A, Colotta F, Donati D, Moll J Cancer Res. 2010 Dec 15;70(24):10255-64. PMID:21159646<ref>PMID:21159646</ref>
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{{ABSTRACT_PUBMED_21159646}}
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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</div>
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==About this Structure==
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<div class="pdbe-citations 2x9e" style="background-color:#fffaf0;"></div>
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[[2x9e]] 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=2X9E OCA].
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==See Also==
==See Also==
*[[Dual specificity protein kinase|Dual specificity protein kinase]]
*[[Dual specificity protein kinase|Dual specificity protein kinase]]
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*[[Dual specificity protein kinase 3D structures|Dual specificity protein kinase 3D structures]]
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==Reference==
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== References ==
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<ref group="xtra">PMID:021159646</ref><references group="xtra"/>
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<references/>
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[[Category: Dual-specificity kinase]]
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__TOC__
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</StructureSection>
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: Avanzi, N.]]
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[[Category: Large Structures]]
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[[Category: Bertrand, J A.]]
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[[Category: Avanzi N]]
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[[Category: Bossi, R T.]]
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[[Category: Bertrand JA]]
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[[Category: Caldarelli, M.]]
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[[Category: Bossi RT]]
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[[Category: Cappella, P.]]
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[[Category: Caldarelli M]]
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[[Category: Colombo, R.]]
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[[Category: Cappella P]]
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[[Category: Colotta, F.]]
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[[Category: Colombo R]]
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[[Category: Cucchi, U.]]
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[[Category: Colotta F]]
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[[Category: Depaolini, S R.]]
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[[Category: Cucchi U]]
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[[Category: Donati, D.]]
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[[Category: DePaolini SR]]
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[[Category: Galvani, A.]]
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[[Category: Donati D]]
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[[Category: Giorgini, M L.]]
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[[Category: Galvani A]]
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[[Category: Isacchi, A.]]
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[[Category: Giorgini ML]]
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[[Category: Mennecozzi, M.]]
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[[Category: Isacchi A]]
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[[Category: Moll, J.]]
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[[Category: Mennecozzi M]]
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[[Category: Perrera, C.]]
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[[Category: Moll J]]
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[[Category: Pesenti, E.]]
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[[Category: Perrera C]]
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[[Category: Rusconi, L.]]
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[[Category: Pesenti E]]
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[[Category: Sola, F.]]
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[[Category: Rusconi L]]
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[[Category: Kinase]]
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[[Category: Sola F]]
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[[Category: Mitotic checkpoint]]
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[[Category: Serine/threonine-protein kinase]]
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[[Category: Transferase]]
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[[Category: Tyrosine-protein kinase]]
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Current revision

HUMAN MPS1 IN COMPLEX WITH NMS-P715

PDB ID 2x9e

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