2x9e

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[[Image:2x9e.png|left|200px]]
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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 [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]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2X9E FirstGlance]. <br>
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</td></tr><tr><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><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><br>
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<tr><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[3hmo|3hmo]], [[3hmp|3hmp]], [[3h9f|3h9f]], [[3hmn|3hmn]], [[3gfw|3gfw]], [[2zmc|2zmc]], [[3cek|3cek]], [[2zmd|2zmd]], [[3dbq|3dbq]]</td></tr>
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<tr><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>
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<tr><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2x9e FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2x9e OCA], [http://www.rcsb.org/pdb/explore.do?structureId=2x9e RCSB], [http://www.ebi.ac.uk/pdbsum/2x9e PDBsum]</span></td></tr>
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<table>
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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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{{STRUCTURE_2x9e| PDB=2x9e | SCENE= }}
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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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===HUMAN MPS1 IN COMPLEX WITH NMS-P715===
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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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{{ABSTRACT_PUBMED_21159646}}
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==About this Structure==
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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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== References ==
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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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__TOC__
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</StructureSection>
[[Category: Dual-specificity kinase]]
[[Category: Dual-specificity kinase]]
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]

Revision as of 00:52, 2 October 2014

HUMAN MPS1 IN COMPLEX WITH NMS-P715

2x9e, resolution 3.10Å

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